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  • Inhibitors & Agonists
    703
    TargetMol | Activity
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    1
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    103
    TargetMol | natural
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    2
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    2
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    103
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    27
    TargetMol | composition
ISOGINKGETIN
4',4'''-Dimethylamentoflavone
T4S21320548-19-6
1. ISOGINKGETIN (4',4'''-Dimethylamentoflavone), a compound derived from the leaves of Ginkgo biloba, to up-regulate adiponectin secretion with potency comparable to that of rosiglitazone, a known modulator of adiponectin production. 2. Isoginkgetin has anti-tumor activity, the mechanistic basis is splicing inhibition , thus, pre-mRNA splicing inhibitors may represent a novel avenue for development of new anti-cancer agents.3. Isoginkgetin can inhibit tumor cell invasion by regulating phosphatidylinositol 3-kinase Akt-dependent matrix metalloproteinase-9 expression. 4. Isoginkgetin (0.3mg kg ip for 3d) can reduce the level of O2·- in plasma and erythroeyte and sometimes increase the activity of SOD in anoxic rats, the action being stronger than aspirin.
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Oleoylestrone
Estrone 3-oleate,MP 101,MP-101,MP101
T28232180003-17-2In house
Oleoylestrone (MP-101) is present in plasma and adipose tissue, has potential antioxidant effects, induces loss of body fat in rats, and can be used for weight loss.
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6-8 weeks
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Methyl eugenol
4-allylveratrole,eugenyl methyl ether,O-methyleugenol,Eugenol Methyl ether
T3S225993-15-2
1. Methyl eugenol (4-allylveratrole) is a natural constituent of the essential oils of a number of plants widely used in foodstuffs as flavouring agents, in view of the carcinogenic potential of ME, the need to check its presence in food products with effective analytical methods. 2. Methyleugenol has insecticidal properties. 3. Methyleugenol can inhibit the production of nitric oxide and decreased the protein expression of inducible nitric oxide synthase, it down-regulates the production of pro-inflammatory cytokines in the ischemic brain as well as in immunostimulated mixed glial cells; indicates that methyleugenol could be useful for the treatment of ischemia inflammation-related diseases. 4. Methyleugenol has cytotoxicity and genotoxicity. 5. Intravenous (i.v.) treatment with methyleugenol (ME) in either anesthetized or conscious rats elicits hypotension, an effect that seems related to an active vascular relaxation rather than withdrawal of sympathetic tone. 6. Methyleugenol has antinociceptive effect on the second phase of formalin-induced pain, may be due to the inhibition of N-methyl-d-aspartic acid (NMDA) receptor-mediated hyperalgesia via GABA(A) receptors. 7. Methyleugenol has elaxant and antispasmodic actions on guinea-pig isolated ileum.
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Sinapinic Acid
Sinapic acid,Synapoic acid
T3753530-59-6
Sinapinic Acid (Synapoic acid) protects the rat liver from CCl4-induced inflammation, most likely by acting as a free radical scavenger and modulator of NF-κB p65 activation and proinflammatory cytokine expression. Sinapic acid with antioxidant role protects cardiac cells and its functions from I R induced oxidative stress. Sinapic acid is a potentially useful agent for the protection against liver fibrosis and cirrhosis. Sinapic acid prevents the alterations in the levels of lipids and lipoproteins by virtue of its anti-lipidaemic effect in isoproterenol induced myocardial infarcted rats. Sinapic acid ameliorates hyperglycemia through PLC-PKC signals to enhance the glucose utilization in diabetic rats.
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Amygdalin
Laetrile
T279529883-15-6
Amygdalin (Laetrile) has antifibrotic, antitumor, anti-inflammatory and analgesic effects, amygdalin joint HSYA could inhibit the degeneration of the endplate chondrocytes derived from intervertebral discs of rats induced by IL-1beta and better than the single use of Amygdalin or HSYA. Amygdalin induces apoptotic cell death in human DU145 and LNCaP prostate cancer cells by caspase-3 activation through down-regulation of Bcl-2 and up-regulation of Bax.
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(S)-Malic acid
L-(-)-Malic acid,(S)-(-)-HYDROXYSUCCINIC ACID,(S)-2-Hydroxysuccinic acid
T483897-67-6
(S)-Malic acid ((S)-2-Hydroxysuccinic acid) is a tart-tasting organic dicarboxylic acid found in many sour foods, such as apples, and contributes to the sourness of green apples and tartness of wine, although its concentration decreases with fruit ripeness (wikipedia). In its ionized form, it is called malate, an intermediate in the TCA cycle alongside fumarate, and can be formed from pyruvate through anaplerotic reactions. In humans, malic acid is derived from food sources and synthesized in the body via the citric acid cycle in mitochondria, playing a crucial role in energy production under both aerobic and anaerobic conditions. Under aerobic conditions, malate is oxidized to oxaloacetate, providing reducing equivalents via the malate-aspartate redox shuttle, while during anaerobic conditions, its simultaneous reduction to succinate and oxidation to oxaloacetate removes excess reducing equivalents, reversing hypoxia’s inhibition of glycolysis and energy production. Studies on rats have shown that tissue malate depletes following exhaustive physical activity, suggesting that malic acid deficiency may cause physical exhaustion. Administering malic acid to rats has been shown to elevate mitochondrial malate, increasing mitochondrial respiration and energy production.
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trans-Cinnamaldehyde
Cinnamaldehyde,Cinnamic aldehyde,Cinnamal,Phenylacrolein
T3S155314371-10-9
1. trans-Cinnamaldehyde (Phenylacrolein) exhibits excellent anti-inflammatory activities and antidepressant-like effects in stressed mid-aged rats as a COX-2 inhibitor. 2. Cinnamic aldehyde induces apoptosis of CML cells in vitro, down-regulation of the expression and function of BCR-ABL may be one of its most important anti-leukemia mechanisms. 3. Cinnamic aldehyde and cinnamic acid are cardioprotective in a rat model of ischemic myocardial injury, the mechanism is related to anti-oxidative and anti-inflammatory properties.
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Triacetonamine hydrochloride
2,2,6,6-Tetramethyl-4-piperidone hydrochloride
TN652133973-59-0
Triacetonamine hydrochloride (2,2,6,6-Tetramethyl-4-piperidone hydrochloride) is an orally available centrally acting depressant compound that can be used as an intermediate for the synthesis of pharmaceutical products and pesticides, and can induce acute liver failure (ALF) in rats.
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Tanshinone IIA sulfonate sodium
Tanshinone IIA sulfonate,Sodium Tanshinone IIA sulfonate,Tanshinone IIA sodium sulfonate,sodium
T294669659-80-9
Tanshinone IIA sulfonate sodium (Tanshinone IIA sodium sulfonate) is a water-soluble derivative of tanshinone IIA extracted from Savia miltiorrhiza; a potent negative allosteric modulator of the human purinergic receptor P2X7. Tanshinone IIA sulfonate sodium (12.5 μM) inhibits hypoxia-induced PKG and PPAR-γ downregulation in PASMCs and distal pulmonary arteries of rats.
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Deltamethrin
Butoss,RU-22974,Esbecythrin,K-Othrin,Decamethrin,RU 22974
T2075452918-63-5
Deltamethrin (RU 22974), a neurotoxic pyrethroid insecticide, produces a reversible sequence of motor symptoms in rats involving hind limb rigidity and choreoathetosis.Deltamethrin is globally used in crop protection, control of malaria and other vector-borne diseases. It is easily degradable.
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Pulegone
(+)-Pulegone
TCS010289-82-7
1. Pulegone ((+)-Pulegone) has cytotoxicity followed by regenerative cell proliferation is the MOA for Pulegone-induced urothelial tumors in female rats. 2. Pulegone induces a verapamil-sensitive psychostimulant effect that appears to independ on the opening of L-type calcium channels. 3. Pulegone has negative reinforcing properties and seems to possess anxiolytic-like actions unrelated to the benzodiazepine site of the γ-aminobutyric acid type A (GABAA) receptor.
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4,6-Benzilidine-D-Glucose
TN721730688-66-5
4,6-Benzilidine-D-Glucose is a clinical antitumor compound showing antitumor activity in rats with chemically induced hepatocellular carcinoma.
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Berberine
Berberin,Umbellatine
T4S07972086-83-1
1. Berberine (Umbellatine) is a potent oral hypoglycemic agent with beneficial effects on lipid metabolism. 2. Berberine may as a broad-spectrum anti-microbial medicine, a complementary therapeutic agent for HIV AIDS. 3. Berberine seems to act as an herbal antidepressant and a neuroprotector against neurodegenerative disorders. 4. Berberine is used in histology for staining heparin in mast cells. As a natural dye, berberine has a colour index of 7516. 5. Berberine reduces hepatic fat content in rats with nonalcoholic fatty liver disease; also prevents proliferation of hepatic stellate cells (HSCs), which are central for the development of fibrosis during liver injury. 6. Berberine can ameliorate proinflammatory cytokines-induced intestinal epithelial tight junction damage in vitro, and berberine may be one of the targeted therapeutic agents that can restore barrier function in intestinal disease states. 7. Berberine has antineoplastic effects, including breast cancer, leukemia, melanoma, epidermoid carcinoma, hepatoma, pancreatic cancer, oral carcinoma, tongue carcinoma, glioblastoma, prostate carcinoma and gastric carcinoma, etc.
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(−)-Myrtenal
(1R)-(−)-Myrtenal
T791218486-69-6
(−)-Myrtenal ameliorates hyperglycemia by enhancing GLUT2 through Akt in the skeletal muscle and liver of diabetic rats.
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Allicin
T3123539-86-6
Allicin exerts antioxidant, bactericidal, anti-cancer, anti-inflammatory activities, it exerts an inhibitory immunomodulatory effect on intestinal epithelial cells. Allicin could significantly inhibit vascular smooth muscle cells' proliferation and migration induced by insulin, which may be related to the inhibition of the activation of ERK signal path. Allicin is beneficial in reducing blood cholesterol, triglycerides levels and systolic blood pressure in hypercholesterolemic rats, it may beneficially affect two risk factors for atherosclerosis-hyperlipidemia and hypertension.
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3,4,5-Trimethoxybenzoic acid
Gallic acid trimethyl ether,Eudesmic acid,Trimethylgallic Acid,Benzoic acid,Tri-O-methylgallic acid
T0632118-41-2
3,4,5-Trimethoxybenzoic acid (Gallic acid trimethyl ether) are potent antioxidants and inhibitor of cytokine production. It can ameliorate chronic stress-induced various behavioral and biochemical alterations in mice. It also exerts hepatoprotective effects in CCl4-induced rats, specifically by modulating oxidative-nitrosative stress and inflammation.
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Sesamol
1,3-Benzodioxol-5-ol,3,4-Methylenedioxyphenol
T3676533-31-3
Sesamol (1,3-Benzodioxol-5-ol) could decrease lung inflammation and lipopolysaccharide (LPS)-induced lung injury in rats. Sesamol ameliorates inflammatory and oxidative damage by upregulating AMPK activation and Nrf2 signaling and blocking the NF-κB and MAPK signaling pathways and inhibits melanin biosynthesis by down-regulating tyrosinase activity and melanin production via regulation of gene expression of melanogenesis-related proteins through modulation of MITF activity, which promotes phosphorylation of p38 and JNK in melan-a cells.
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(R)-5-Oxopyrrolidine-2-carboxylic acid
D-Pyroglutamic acid,(R)-(+)-2-Pyrrolidone-5-carboxylic acid
T48144042-36-8
(R)-5-Oxopyrrolidine-2-carboxylic acid (D-Pyroglutamic acid) is a cyclic derivative of glutamic acid, physiologically present in mammalian tissues. It releases GABA from the cerebral cortex and exhibits anti-anxiety effects in a simple approach-avoidance conflict situation in rats. In clinical pharmacology experiments, it significantly shortens the plasma half-life of ethanol during acute intoxication.
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Harmaline hydrochloride
Harmidine hydrochloride
T8769363-11-1
Harmaline hydrochloride (Harmidine hydrochloride) is a fluorescent indole alkaloid from the group of harmala alkaloids and beta-carbolines. It is the partially hydrogenated form of harmine.Harmaline produces a generalized tremor in normal rats by inducing rhythmic firing of inferior olivary neurons
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N,N'-Dimethylthiourea
DMTU
T40615534-13-4
N,N'-Dimethylthiourea (DMTU) (DMTU), isolated from Allii Sativi Bulbus, is an orally active scavenger of hydroxyl radical ( OH) and blocks OH production by activated neutrophils in vitro. N,N'-Dimethylthiourea protects against water-immersion restraint stress (WIRS)-induced gastric mucosal lesions in rats by exerting its antioxidant action including OH scavenging and anti-inflammatory action [1][2] .
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PACAP (1-27), human, ovine, rat acetate
PACAP 1-27 acetate,PACAP (1-27), human, ovine, rat acetate(127317-03-7 free base)
TP1070L
PACAP (1-27), human, ovine, rat acetate (PACAP 1-27 acetate) is a novel neuropeptides originally isolated from bovine hypothalamus, also found in humans and rats.
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Simmondsin
TN676451771-52-9
Simmondsin is a natural product from Simmondsia chinensis -- jojoba. It reduced food intake and body weight without apparent negative effects in rats.
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D-Mannoheptulose
T109403615-44-9In house
D-mannoheptose is the main non-structural carbohydrate in avocado. D-mannoheptose is a specific inhibitor of D-glucose phosphorylation. D-mannoheptose can prevent the release of insulin and the utilization of carbohydrates in rats.
    7-10 days
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    Calenduloside E
    Silphioside F
    TJS092826020-14-4
    Calenduloside E (Silphioside F) exhibits hypoglycemic activities by suppressing the transfer of glucose from the stomach to the small intestine and by inhibiting glucose transport at the brush border of the small intestine in oral glucose-loaded rats.
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    Polygalasaponin F
    T3826882664-74-6
    Polygalasaponin F has anti-neuroinflammatory activity, can inhibit the release of inflammatory cytokines TNF-α and NO induced by lipopolysaccharides (LPS) and reduce the expression of inducible nitric oxide synthases. Polygalasaponin F can significantly i
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    Alnustone
    (4E,6E)-1,7-Diphenyl-4,6-heptadien-3-one
    T4S017633457-62-4
    Alnustone ((4E,6E)-1,7-Diphenyl-4,6-heptadien-3-one) exerts significant anti-inflammatory activity in the assay of carrageenin-induced hind paw edema in rats.
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    Shogaol
    [6]-Shogaol,6-Shogaol
    T6S1699555-66-8
    1. 6-Shogaol (6-Shogaol) has antipyretic and analgesic effects in addition to inhibitory effect on lipoxygenase activity. 2. 6-shogaol has anti-inflammatory property, reduces the inflammatory response and protected the femoral cartilage from damage produced in a CFA monoarthritic model of the knee joint of rats. 3. 6-Shogaol inhibits the growth of human cancer cells and induces apoptosis in COLO 25 cells through modulation of mitochondrial functions regulated by reactive oxygen species (ROS). 4. 6-Shogaol effectively inhibit invasion and metastasis of hepatocellular carcinoma through diverse molecular mechanisms, including inhibition of the MAPK and PI3k Akt pathways and NF-κB and STAT3 activities to suppress expression of MMP-2 -9 and uPA and block angiogenesis, could further regulate urokinase-type plasminogen activity.
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    Linarin
    Buddleoflavonoloside,Buddleoside,Acacetin-7-O-rutinoside,Acaciin,Linarine
    T6S0653480-36-4
    1. Linarin (Acacetin-7-O-rutinoside) (acacetin-7-O-β-d-rutinoside) shows selective dose dependent inhibitory effect on acetylcholinesterase. 2. Linarin alleviates GalN LPS-induced liver injury by suppressing TNF-α-mediated apoptotic pathways. 3. Linarin prevents A beta-induced neurotoxicity through the activation of PI3K Akt, which subsequently inhibits GSK-3b and up-regulates Bcl-2. 4. The piperine significantly enhanced the oral absorption of Linarin in rats by inhibiting P-glycoprotein mediated cellular efflux during the intestinal absorption and likely simultaneously by inhibiting the metabolism of Linarin.
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    Bilobetin
    T4S2128521-32-4
    Bilobetin ameliorates insulin resistance by PKA-mediated phosphorylation of PPARα in rats fed a high-fat diet.
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    3,4-O-Isopropylidene-shikimic acid
    3,4-O-Isopropylidene shikimic acid
    TN1238183075-03-8
    3,4-O-Isopropylidene-shikimic acid (3,4-O-Isopropylidene shikimic acid) exhibits significant anti-inflammatory, anti-thrombosis, antioxidant, and analgesic effects, and provides protective benefits against trinitrobenzenesulfonic acid-induced experimental colitis in rats, likely because of its antioxidant properties.
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    Taurodeoxycholic acid sodium hydrate
    Sodium taurodeoxycholate monohydrate,Taurodeoxychloic Acid sodium hydrate,Taurohyodeoxycholic acid sodium salt
    TJA2398110026-03-4
    Taurodeoxycholic acid sodium hydrate (Sodium taurodeoxycholate monohydrate), a hydrophilic bile salt, influences bile salt and biliary lipid secretion in rats.
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    taraxasteryl acetate
    T57816426-43-3
    Taraxasterol acetate has anti-inflammatory activity in bino rats against carrageenan, formaldehyde and adjuvant induced inflammations. Taraxasterol acetate also displays potential antibacterial activities.
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    Crocin II
    Crocin 2,Crocetin gentiobiosylglucosyl ester,Tricrocin,Crocin B
    T377955750-84-0
    Crocin II (Crocetin gentiobiosylglucosyl ester) has anti-inflammatory and anti-apoptotic effects against gastric ischemia-reperfusion injury in rats, the effect of crocin is mainly mediated by reducing the protein expression of iNOS and caspase-3. Crocin II can ameliorate CCl4-induced liver injury via inhibition of inflammatory cytokines, caspase3 and oxidative stress along with modulation of liver metabolizing enzymes favoring elimination of CCl4 toxic metabolite. Crocin II has antihyperlipidemic effect, may be due to the inhibition of pancreatic lipase and crocin, and its metabolite, Crocin II , can improve hyperlipidemia. Crocin has antidepressant effects by increasing CREB, BDNF and VGF levels in hippocampus.
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    Harzianopyridone
    (-)-Harzianopyridone
    TN7266137813-88-8
    Harzianopyridone is an atpenin-like compound that functions as an inhibitor of mammalian and nematode mitochondrial complex II, also known as succinate:ubiquinone oxidoreductase (SQR), demonstrating IC50 values of 0.017, 0.2, and 2 μM against bovine, rat, and nematode complex II, respectively. Additionally, it inhibits nematode quinol-fumarate reductase (QFR) with an IC50 value of 0.36 μM. Significantly selective for complex II over complexes I and III in rats and cattle, as well as complex I in nematodes, with IC50 values exceeding 100 μM, it exhibits notable antibacterial and antifungal properties, with EC50 values of 35.9, 42.2, 60.4, and 50.2 μg/ml against R. solani, S. rolfsii, M. phaseolina, and F. oxysporum, respectively.
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    Rhodiocyanoside A
    TN2155168433-86-1
    Rhodiocyanoside A has antiallergic activity, it exhibits inhibitory activity on the histamine release from rat peritoneal exudate cells sensitized with anti-DNP IgE and inhibits the PCA reaction in rats.
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    Globularin
    TN41381399-49-1
    Globularin has hypoglycaemic and hypolipidemic activities in normal and streptozotocin-induced diabetic rats.
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    3alpha-dihydrocadambine
    TN299054483-84-0
    3alpha-Dihydrocadambine exhibits dose-dependent hypotensive and anti-hypertensive effects in anesthetized normotensive rats and in conscious spontaneously hypertensive rats.
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    Escin IIB
    TN1623158800-83-0
    Escin IIB has positive effects on acute inflammation in animals, it can inhibit the induced by serotonin in rats, the hind paw edema induced by carrageenin, and the scratching behavior induced by compound 48 80 in mice.
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    Kinsenoside
    (+)-Kinsenoside
    T3849151870-74-5
    Kinsenoside ((+)-Kinsenoside) shows significant antihepatotoxic, and anti-inflammatory activities. Kinsenoside could be useful for repairing beta cells in pancreatic islet injury as well as improving its function, it could promote the glucose tolerance of acute glucose increase in both diabetic and normal healthy rats. Kinsenoside inhibits osteoclastogenesis from macrophages by attenuating RANKL-induced NF-κB and NFATc1 activities, which in turn, prevents bone loss from OVX mice.
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    Nicotiflorin
    Nictoflorin,Kaempferol-3-O-Rutinoside,Nicotifloroside
    T6S129417650-84-9
    1. Nicotiflorin (Kaempferol-3-O-Rutinoside) has potential therapeutic effects on cerebral ischemic illness. 2. Nicotiflorin has protective effects on reducing memory dysfunction, energy metabolism failure and oxidative stress in multi-infarct dementia model rats.
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    Propylparaben sodium
    Propyl4-hydroxybenzoatesodium,Propylparahydroxybenzoatesodium
    T4044235285-69-9
    Propylparaben sodium (propyl parahydroxybenzoate) is a naturally occurring antimicrobial preservative found in plants and bacteria. Widely utilized in cosmetics, pharmaceuticals, and foods, this compound impairs antral follicle growth and steroidogenic function by modifying the cell-cycle, apoptosis, and steroidogenesis pathways. Additionally, propylparaben sodium reduces sperm count and motility in rats.
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    7-10 days
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    Nantenine
    TN46242565-01-7
    Nantenine is an acetylcholinesterase inhibitor, it functions as an effective antagonist against a wide range of MDMA-induced effects in mice. Nantenine has anticonvulsant effect, which seems attributable to its stimulation and the resultant decrease of Ca
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    Luvangetin
    TN4465483-92-1
    Luvangetin may have anti-inflammatory activity, it can inhibit NO and PGE2 production in LPS-stimulated BV2 cells. Luvangetin shows significant protection against pylorus-ligated and aspirin-induced gastric ulcers in rats and cold restraint stress-induced
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    7-10 days
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    1-Stearoyl-rac-glycerol
    Glyceryl monostearate,Monostearin
    T36454123-94-4
    1-Stearoyl-rac-glycerol is a monoacylglycerol that contains stearic acid at the sn-1 position. 1-Stearoyl-rac-glycerol levels are decreased in tumor tissue in a mouse model of azoxymethane-induced colorectal carcinogenesis. 1-Stearoyl-rac-glycerol has been used in the composition of transfersomes for transdermal delivery of doxorubicin in rats, leading to doxorubicin accumulation in lymph nodes, spleen, and heart.
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    3',6-Disinapoylsucrose
    Disinapoyl sucrose,3,6'-Disinapoyl sucrose
    T3697139891-98-8
    3',6-Disinapoylsucrose (Disinapoyl sucrose) shows the neuroprotective effect and antidepressive activity in rats.
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    alpha-Tocopherolquinone
    Metarene
    T70507559-04-8
    During hypoxia in rats, levels of α-tocopherylquinon have been found to rise. alpha-Tocopherolquinone (Metarene) is reported to downregulate the respiratory activity of mitochondria. alpha-Tocopherolquinone has also displayed antioxidant activities after it is reduced to tocopherylhydroquinone.
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    Pachypodol
    TN203233708-72-4
    Pachypodol, a methoxyflavonoid isolated from Pogostemon cablin Bentham, has antioxidant and cytoprotective properties and inhibits the growth of CaCo 2 colon cancer cell lines in vitro.Pachypodol protects neonatal rats from anesthesia-induced apoptosis in the developing brain through modulation of the JNK ERK pathway.PDGFRα kinase inhibitory activity in macrophages exposed to STING agonists.
      7-10 days
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      CLINODISIDE A
      T3875916347-31-4
      Clinodiside A in rats with one compartment open model into the body, rapid distribution, elimination rate.
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