Gemfibrozil (CI-719) interacts with peroxisome proliferator-activated receptors (PPARalpha) resulting in PPARalpha-mediated stimulation of fatty acid oxidation and an increase in lipoprotein lipase (LPL) synthesis. Gemfibrozil is a fibric acid derivative with hypolipidemic effects. This enhances triglyceride-rich lipoprotein clearance and reduces the expression of apolipoprotein C-III (apoC-III). The reduction in hepatic production of apoC-III result in the subsequent reduction of serum levels of very-low-density-lipoprotein cholesterol (VLDL-C). In addition, gemfibrozil-mediated PPARalpha stimulation of apoA-I and apoA-II expression results in an increase in high-density lipoprotein cholesterol (HDL-C).

Vardenafil (Vivanza) is an oral therapy for the treatment of erectile dysfunction. It is a selective inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5). Penile erection is a hemodynamic process initiated by the relaxation of smooth muscle in the corpus cavernosum and its associated arterioles. During sexual stimulation, nitric oxide is released from nerve endings and endothelial cells in the corpus cavernosum. Nitric oxide activates the enzyme guanylate cyclase resulting in increased synthesis of cyclic guanosine monophosphate (cGMP) in the smooth muscle cells of the corpus cavernosum. The cGMP in turn triggers smooth muscle relaxation, allowing increased blood flow into the penis, resulting in erection. The tissue concentration of cGMP is regulated by both the rates of synthesis and degradation via phosphodiesterases (PDEs). The most abundant PDE in the human corpus cavernosum is the cGMPspecific phosphodiesterase type 5 (PDE5); therefore, the inhibition of PDE5 enhances erectile function by increasing the amount of cGMP.

Cepharanthine (NSC-623442), a biscoclaurine alkaloid, suppresses tumor necrosis factor (TNF)-α-mediated NFκB stimulation, plasma membrane lipid peroxidation and platelet aggregation and inhibits cytokine production.

Arecoline hydrobromide (Arecoline HBr) is a muscarinic acetylcholine receptor agonist.

Bisdemethoxycurcumin (Curcumin III) is a natural demethoxy derivative of curcumin. It is a potent activator of macrophage phagocytosis, interacting with 1α, 25-dihydroxy vitamin D3 to stimulate amyloid-β clearance by macrophages (optimal stimulation at 100 nM BDMC) [1]. More stable than curcumin in physiological media, BDMC suppresses proliferation of cancer cells [2]. It down-regulates the transcriptional coactivator p300, suppressing the Wnt/β-catenin pathway, and inhibits LPS induction of iNOS expression [3].

Vardenafil hydrochloride is a New Phosphodiesterase Type 5(PDE5) Inhibitor, in the Treatment of Erectile Dysfunction in Men With Diabetes

5-Hydroxy-1-methylhydantoin (HD-003) is an antioxidant potentially for the treatment of renal failure. A creatinine metabolite, 5-Hydroxy-1-methylhydantoin , a hydroxyl radical scavenger, has previously been shown to confer renoprotection by inhibiting the progression of chronic kidney disease in rats. 5-Hydroxy-1-methylhydantoin is a novel anti-oxidant drug completely suppressed the expression of B2-kinin receptors (B2KR) in response to high glucose (25 mM) stimulation in VSMC and was also shown to attenuate the effects of BK on VSMC remodeling. 5-Hydroxy-1-methylhydantoin inhibited the BK-induced increase in MAPK phosphorylation and attenuated the increase in connective tissue growth factor (CTGF) protein levels in VSMC. These findings suggest that 5-Hydroxy-1-methylhydantoin may confer vascular protection against high glucose concentrations and BK-stimulation to ameliorate vascular injury and remodeling through its anti-oxidant properties.

Ac-RYYRIK-NH2 acetate is an agonist at nociceptin/orphanin FQ(noc/OFQ) receptors, affecting spontaneous locomotor activity. Ac-RYYRIK-NH2 acetate is a partial agonist on ORL1 transfected in CHO cells, antagonizes the stimulation of [35S]-GTPgammaS binding to G proteins by noc/OFQ in membranes and sections of rat brain.

Compound 1T-0216 is a blocker of AKT1-FAK interactions and reduces stimulation of FAK phosphorylation by extracellular stress in human SW620 colon cancer cells without affecting basal FAK phosphorylation.

Triptorelin acetate(57773-63-4 free base) (CL 118,532) is used as a GnRH agonist. It decreases pituitary secretion of gonadotropins luteinizing hormone (LH) and follicle-stimulating hormone (FSH) by causing constant stimulation of the pituitary. Triptorelin acetate(57773-63-4 free base) may be used in the treatment of hormone-responsive cancers such as breast cancer or prostate cancer, precocious puberty, estrogen-dependent conditions, and assisted reproduction.

Acetyl tetrapeptide-9 Acetate plays a role in the stimulation of basement membrane polysaccharide (lumican) and the synthesis of collagen I.

Kisspeptin 234 acetate(1145998-81-7 free base) is a Kisspeptin receptor (KISS1, GPR54) antagonist; a Kisspeptin-10 analogue. It inhibits the stimulation of inositol phosphate (IP) (IC50 = 7 nM) and the release of gonadotropin-releasing hormone (GnRH) by kisspeptin-10.

KW-2450 free base is an orally bioavailable inhibitor of insulin-like growth factor 1 receptor (IGF-1R) and insulin receptor (IR) tyrosine kinases with potential antineoplastic activity. IGF-1R/IR inhibitor KW-2450 free base selectively binds to and inhibits the activities of IGF-1R and IR, which may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. IGF-R1 and IR tyrosine kinases, overexpressed in a variety of human cancers, play significant roles in the stimulation of cellular proliferation, oncogenic transformation, and suppression of apoptosis.

Compound 1T-0219 (SC) is a blocker of AKT1-FAK interaction reducing the stimulation of FAK phosphorylation in response to extracellular pressure in human SW620 colon cancer cells without affecting basal FAK phosphorylation.

VA-K-14 hydrochloride（VAK14 HCl） is a selective thyrotropin receptor (TSHR) antagonist (IC50= 12.3 μM) that inhibits TSHR stimulation by serum and monoclonal TSHR-stimulating antibodies from patients with GD and abrogates TSHR signaling.

Atropine (DL-Hyoscyamine) Sulfate is the sulfate salt of atropine, a naturally-occurring alkaloid isolated from the plant Atropa belladonna. Atropine functions as a sympathetic, competitive antagonist of muscarinic cholinergic receptors, thereby abolishing the effects of parasympathetic stimulation.

1. β-Anhydroicaritin exhibits immunosuppressive effect on the mouse macrophages stimulated by LPS. 2. β-Anhydroicaritin phytosomes can inhibit enhanced bone turnover induced by ovariectomy, improve BMD the biomechanical properties of vertebrae, without any stimulation on uterus. 3. β-Anhydroicaritin possesses significant protective effects on the zymosan-induced peritonitis mice, which might be associated with the regulation of Ca(2+); influx in macrophages and iNOS expression.

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

Vardenafil dihydrochloride (Levitra) is a new type PDE inhibitor with IC50 of 0.7 and 180 nM for PDE5 and PDE1, respectively.

XY-52 (Compound 32), an ST2 (Stimulation-2) inhibitor, exhibits IC50 values of 5.68 μM and 4.59 μM in the AlphaLISA and HEK-Blue assays, respectively. It promotes proinflammatory T-cell proliferation and diminishes plasma sST2 and IFNγ biomarkers in a graft versus host disease (GVHD) mouse model [1].

Peptide 12d, an antimicrobial peptide derived from wasp venom, induces antimicrobial effects through the stimulation of mast cell degranulation [1].

Lorukafusp alfa (14.18 mAb; hu14.18-IL2) is an immunocytokine composed of the humanized 14.18 anti-GD2 monoclonal antibody (mAb) connected to interleukin-2 (IL210). It exerts its anti-tumor effects [1] through the induction of antibody-dependent cellular cytotoxicity (ADCC) and complement-dependent cytotoxicity. This is achieved by the targeted binding of hu14.18-IL2 to GD2-expressing tumor cells, which facilitates subsequent interaction with Fc receptors on immune effector cells, as well as the stimulation of natural killer (NK) and T cells through their IL2 receptors.

Mabuterol is a selective agonist of β2 adrenoreceptor with no beta 1-stimulation. Mabuterol inhibited the positive inotropic effect of isoprenaline at 10(-7) g/ml and decreased the maximum driving frequency at 3 X 10(-6) g/ml. Mabuterol was 3 times more p

Abatacept (CTLA4lg) is a soluble fusion protein consisting of the extracellular domain of human CTLA4 and a fragment of the Fc portion of human IgG1 (hinge and CH2 and 3 domains). It is a selective T-cell co-stimulation modulator and a protein drug for au

Leukotriene B4 (LTB4) is a dihydroxy fatty acid derived from arachidonic acid through the 5-LO pathway. It promotes a number of leukocyte functions including aggregation, stimulation of ion fluxes, enhancement of lysosomal enzyme release, superoxide anion production, chemotaxis, and chemokinesis. 12-oxo LTB4 is an initial metabolite of LTB4 formed via the LTB4 12-hydroxydehydrogenase pathway. It is rapidly converted to 10,11-dihydro-12-oxo-LTB4, followed by reduction of the 12-oxo group to give 10,11-dihydro-LTB4. 12-oxo-LTB4 (EC50 = 33 nM) is about 70-fold less potent than LTB4 (EC50 = 0.46 nM) at stimulating Ca2+ mobilization in human neutrophils. It is also significantly less potent than LTB4 at stimulating neutrophil migration with EC50 values of 170 and 2.7 nM for 12-oxo-LTB4 and LTB4, respectively.

PAF C-18 is a naturally occurring phospholipid produced upon stimulation through two distinct pathways known as the remodeling and 'de novo' pathways. It is less potent than PAF C-16 in the induction of platelet aggregation

(±)14-HDHA is an autoxidation product of docosahexaenoic acid (DHA) in vitro. It is also produced from incubations of DHA in rat liver, brain, and intestinal microsomes. DHA is metabolized to 14(S)-HDHA by human platelets along with 11(S)-HDHA. 14(S)-HDoHE is also produced by salmon gills upon stimulation with calcium ionophore. 14(S)-HDHA was shown to be an inhibitor of U-46619-induced human platelet aggregation and rabbit and rat aortic smooth muscle contraction with IC50 values of about 70, 3.6, and 5.3 μM, respectively. (±)14-HDHA is a potential marker of oxidative stress in brain and retina where DHA is an abundant polyunsaturated fatty acid.

Electrolyte and fluid transport in the kidney are regulated in part by arachidonic acid and its metabolites. 16-HETE is a minor CYP450 metabolite of arachidonic acid released by the kidney upon angiotensin II stimulation that demonstrates stereospecific biological activity. Electrolyte and fluid transport in the kidney are regulated in part by arachidonic acid and its metabolites. 16-HETE is a minor CYP450 metabolite of arachidonic acid released by the kidney upon angiotensin II stimulation that demonstrates stereospecific biological activity. 16(S)-HETE inhibits proximal tubule ATPase activity by as much as 60% at a concentration of 2 µM.[1]

Kisspeptin 234 is a kisspeptin receptor (KISS1, GPR54) antagonist; kisspeptin-10 analog. Inhibits kisspeptin-10 stimulation of inositol phosphate (IP) (IC50 = 7 nM) and release of gonadotrophin-releasing hormone (GnRH).

QL-1200186 is an orally active, selective TYK2 inhibitor that, upon dose-dependent oral administration, suppresses interferon-γ (IFNγ) production following interleukin-12 (IL-12) stimulation and markedly improves skin lesions in a psoriatic mouse model [1].

4-epi-Withaferin A (compound 28), an analogue of Withaferin A, exhibits enhanced cytotoxicity and cytoprotective heat-shock-inducing activity (HSA). It shows promise for the investigation of protein aggregation-associated diseases through the stimulation of cellular defense mechanisms [1].

AP 811 acetate is a selective antagonist of the atrial natriuretic peptide clearance receptor (ANP-CR, NPR3), demonstrating high affinity with a K_i value of 0.48 nM and exhibiting over 20,000-fold selectivity for NPR3 compared to NPR1. It effectively inhibits ANP-induced pump stimulation [1] [2].

AP 811, a selective antagonist of the atrial natriuretic peptide clearance receptor (APN-CR, NPR3) with a K i value of 0.48 nM, exhibits remarkable selectivity for NPR3 over NPR1 by more than 20,000-fold. Moreover, AP 811 effectively eliminates ANP-induced pump stimulation.

Prazobind is a prazosinoid substance that blocks insulin stimulation of IP1 (inositol phosphate) accumulation and is an effective α1 adrenoceptor blocker.

Ciprofibrate impurity A is an impurity of Ciprofibrate. Ciprofibrate is a PPARα agonist[1]. [1]. Passilly, P., et al., Phosphorylation of peroxisome proliferator-activated receptor alpha in rat Fao cells and stimulation by ciprofibrate. Biochem Pharmacol, 1999. 58(6): p. 1001-8.

Cyclomorusin exhibits competitive inhibition toward monophenolase activity of mushroom tyrosinase, the IC50 value of 0.092 microM. It evokes the stimulation of superoxide anion generation in fMLP-stimulated rat neutrophils. Cyclomorusin , neocyclomorusin

Cucurbitacin I, cytotoxic triterpenoid sterols isolated from plants, elicits the formation of actin/phospho-myosin II co-aggregates by stimulation of the RhoA/ROCK pathway and inhibition of LIM-Kinase.

Electrolyte and fluid transport in the kidney are regulated in part by arachidonic acid and its metabolites. (±)16-HETE is the racemic version of a minor CYP450 metabolite of arachidonic acid released by the kidney upon angiotensin II stimulation. The biological activity of 16-HETE is stereospecific. 16(R)-HETE dose-dependently stimulates vasodilation of the rabbit kidney, however 16(S)-HETE does not affect perfusion pressure. At a concentration of 2 μM the (S)-enantiomer of 16-HETE inhibits proximal tubule ATPase activity by as much as 60%, whereas the (R)-isomer has negligible effects on ATPase activity.

(D-Arg1,D-Pro2,D-Trp7,9,L-Leu11)-Substance P (acetate), an antagonist for Substance P and Bombesin, modulates ocular inflammatory responses triggered by antidromic trigeminal nerve stimulation [1].

γ-Bag cell peptide, a peptide situated near the N-terminus of the egg-laying prohormone, is released from vesicles upon insulin stimulation. It is utilized in research pertaining to both the central and peripheral nervous systems [1].

Competence-Stimulating Peptide-12261 acetate is a fragment of sensory stimulation peptide, which is a quorum sensing molecule that inhibits germ tube (GT) formation

Electrolyte and fluid transport in the kidney are regulated in part by arachidonic acid and its metabolites. 16-HETE is a minor CYP450 metabolite of arachidonic acid released by the kidney upon angiotensin II stimulation that demonstrates stereospecific biological activity. 16(S)-HETE inhibits proximal tubule ATPase activity by as much as 60% at a concentration of 2 μM.

Palmitoyl-L-aspartic acid is a natural N-acylaspartate that suppresses Hedgehog signaling after stimulation with Smoothened agonist or non-sterol-modified Sonic Hedgehog. It does not alter the activity of cannabinoid receptors or fatty acid amide hydrolas

(±)-2'-Hydroxy Ceramide (d18:0/18:0) is a sphingomyelin derivative isolated from mammalian platelets upon ADP stimulation [1].

Naratriptan Hydrochloride is the hydrochloride salt form of naratriptan, a sulfonamide with selective serotonin (5-HT) 1 receptor agonistic activity and anti-migraine property. Naratriptan hydrochloride (GR-85548A hydrochloride) binds selectively and with high affinity to the 5-HT1D and 5-HT1B receptor subtypes. Activation of these 5-HT1D/B receptors located on intracranial blood vessels leads to vasoconstriction and provides relief of migraine headaches. Naratriptan hydrochloride may also exerts its effect by stimulation of 5-HT1D/1B receptors on sensory nerve endings in the trigeminal system thereby decreasing the release of pro-inflammatory neuropeptides.

Amezinium methylsulfate (Lu-1631) has multiple mechanisms, including stimulation of alpha and beta-1 receptors and inhibition of noradrenaline and tyramine uptake.

Addition of the Rhamnose (6-Deoxy-L-mannose)-rich polysaccharide, RROP-1, to normal human dermal fibroblasts (NHDFs) and human endothelial cells produced a dose-dependent stimulation of the calcium-signaling pathway, inducing fast and transient increases in Ca2 influx and intracellular free Ca2 level.

Xamoterol hemifumarate is a potent and selective β1-adrenoceptor agonist.Xamoterol hemifumarate is a potential compound for the study of the relationship between cardiac arrhythmias and β1-adrenergic stimulation with IKr.

1. Apiin (Apioside) is the reducing and stabilizing agent. 2. Apiin has inhibitory activity in-vitro on iNOS expression and nitrite production when added before LPS stimulation in the medium of J774.A1 cells.