free fatty acid receptor

VCH-916 is a novel nonnucleoside HCV NS5B polymerase inhibitor.

Quilseconazole Formic acid is a selective inhibitor of fungal Cyp51 with potent activities against Cryptococcus neoformans and Cryptococcus gattii.

Mavodelpar free acid hydrochloride (Pparδ agonist HCl) is a potent PPARδ agonist.

GSK2983559 free acid is an effective and selective inhibitor of receptor-interacting protein 2 (RIP2). GSK2983559 free acid shows excellent activity in blocking many proinflammatory cytokine responses in human inflammatory bowel disease explant samples an

AM095 (free acid) is a potent LPA1 receptor antagonist with IC50 values of 0.98 μM for recombinant human LPA1 and 0.73 μM for recombinant mouse LPA1.

E-3030 free acid is a peroxisome proliferator-activated receptor (PPAR) agonist. E-3030 decreased blood glucose, triglyceride, non-esterified fatty acids, and insulin levels and increased blood adiponectin levels. Triglyceride- and non-high-density lipopr

Zomepirac is a prostaglandin synthetase inhibitor. Zomepirac is an orally effective nonsteroidal anti-inflammatory drug (NSAID) that has antipyretic actions.

CI-959 Free Acid is an orally effective inhibitor of cell activation in vitro and in animal models and also has anti-allergic/anti-inflammatory properties.

KRH-594 is a potent, specific and insurmountable AT1 receptor antagonist. KRH-594 ameliorates hyperlipidaemia and nephropathy in diabetic spontaneously hypertensive rats. KRH-594 prevents end-organ damage in stroke-prone spontaneously hypertensive/Izm ra

RDEA-806, a reverse transcriptase inhibitor, is used potentially for the treatment of HIV infection.

Gastrazole is a CCK2 receptor antagonist potentially. It also used for the treatment of pancreatic cancer.

IQ-1S free acid (IQ-1S) is an effective and specific c-Jun N-Terminal Kinase Inhibitor. IQ-1S inhibits murine delayed-type hypersensitivity. IQ-1S can reduce inflammation and cartilage loss associated with CIA and can serve as a small-molecule modulator for mechanistic studies of JNK function in rheumatoid arthritis. IQ-1S is highly specific for JNK and that its neutral form is the most abundant species at physiologic pH.

AM-643 Free Acid is a bio-active chemical.

AFP 07 free acid is a 7,7-difluoroprostacyclin derivative. It also acts as a selective and highly potent agonist for the IP receptor.

AM-103 Free Acid is a bio-active chemical.

Minnelide is an effective therapy against pancreatic cancer. Minnelide Inhibits Androgen Dependent, Castration Resistant Prostate Cancer Growth by Decreasing Expression of Androgen Receptor Full Length and Splice Variants. Minnelide reduced tumor volume in multiple models of pancreatic cancer. Minnelide was a more effective drug against pancreatic cancer models. It effectively reduced tumor burden and tumor related morbidity in different unique but complementary mouse models. It reduced metastatic spread and increased survival in the different models as well.

AVE-1330A free acid is a broad-spectrum non-beta-lactam beta-lactamase inhibitor.

Cefcanel is a semisynthetic third-generation cephalosporin with antibacterial activity. Cefcanel is active against the species E. coli, K. aerogenes and Proteus mirabilis; H. influenzae and M. catarrhalis has reasonable susceptibility. Cefcanel inhibits 90% of S. aureus strains at 2 µg/ml, irrespective of the presence of a β-lactamase. Cefcanel binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. PBPs are enzymes involved in the terminal stages of assembling the bacterial cell wall and in reshaping the cell wall during growth and division. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This results in the weakening of the bacterial cell wall and causes cell lysis.

Oxytocin free acid, also known as 9-Deamidooxytocin, is an analog of oxytocin where the glycinamide residue at position 9 has been substituted with a glycine residue. Oxytocin, a pleiotropic peptide hormone, has wide-ranging implications for general health, adaptation, development, reproduction, and social behavior.

Talaporfin, an effective tumor localizer, can produce the selective degradation of tumor tissue following light exposure.

(D-Trp6)-LHRH free acid is a luteinizing hormone-releasing hormone (LHRH) agonist [1].

Myristoyl-(Lys12,27,28)-VIP-Gly-Gly-Thr (free acid) acts as a selective and potent antagonist of the VPAC2 receptor [1].

Substance P, Free Acid, is a synthetic analog of native Substance P but lacks its biological activity.

Urocortin III (mouse) (free acid), a selective high-affinity agonist for the CRF2 receptor, significantly inhibits gastric emptying without affecting colonic transit [1] [2].

4-Methylumbelliferyl-α-L-iduronide (free acid) is a fluorogenic substrate for α-L-iduronidase, an enzyme found in cell lysosomes that is involved in the degradation of glycosaminoglycans such as dermatan sulfate and heparin sulfate. 4-Methylumbelliferyl-α-L-iduronide is cleaved by α-L-iduronidase to release the fluorescent moiety 4-methylumbelliferyl (4-MU). 4-MU fluorescence is pH-dependent with excitation maxima of 320 and 360 nm at low (1.97-6.72) and high (7.12-10.3) pH, respectively, and an emission maximum ranging from 445 to 455 nM, increasing as pH decreases. This substrate is used in assays that measure the activity of α-L-iduronidase, which is commonly deficient in a type of lysosomal storage disease called mucopolysaccharidosis.

PA22-2 (free acid) (Cys-Laminin A chain 2091-2108), a peptide, promotes neurite outgrowth and facilitates the formation of neuron-like processes. It is used in the culturing of human adenoid cystic carcinoma cells and the development of peptide-functionalized supported phospholipid bilayers [1] [2] [3].

Cefpodoxime (free acid) is an oral, third-generation cephalosporin antibiotic. It is active against most Gram-positive and Gram-negative organisms, except Pseudomonas aeruginosa, Enterococcus, and Bacteroides fragilis.

SR-717 free acid is a stable cGAMP mimetic and non-nucleotide STING agonist, demonstrating antitumor activity with EC50 values of 2.1 μM in ISG-THP1 (WT) and 2.2 μM in ISG-THP1 cGAS KO (cGAS KO) cell lines.

Tiron free acid is a bioactive chemical.

NK-611 free acid is a new semisynthetic analogue of etoposide, which presumably also acts through inhibition of topoisomerase II, and has been found to be more potent against several cancer cell lines in vitro than etoposide.

CGP-75254A Free Acid is a novel oral iron chelator.

SSR128129E (free acid) is an orally available, allosteric inhibitor of FGFR, with an IC50 of 1.9 μM for FGFR1.

YCT529 free acid is a potent, selective, and orally active RAR-α inhibitor.

15-keto Latanoprost is a potential metabolite of latanoprost when administered to animals and is a common minor impurity in commercial preparations of the bulk drug compound. Although much less potent than latanoprost, 15-keto Latanoprost can still produce a small but measurable decrease (1 mm Hg) in intraocular pressure in normal cynomolgus monkeys at a dose of 1 μg eye. It also acts as a miotic in normal cats, causing an 8 mm Hg reduction in pupillary diameter at 5 μg eye, though it is not as potent as many other F-type prostaglandins, such as prostaglandin F2α, which achieves the same effect at less than 1 μg eye.

ADRA1D receptor antagonist 1 (free base), an antagonist with a K_i value of 1.6 nM, dose-dependently inhibits bladder contraction with an IC_30 value of 15 nM. It is useful in studies of overactive bladder disorders such as urinary urgency, frequency, and incontinence.

Melittin free acid, a basic 26-amino-acid polypeptide, constitutes the primary active component of honeybee venom and serves as a phospholipase A2 (PLA2) activator. Exhibiting a broad-spectrum antifungal effect, it presents MIC values ranging from 0.4-60 μM. Its mechanism includes inducing cell apoptosis, inhibiting (1,3)-β-D-glucan synthase, and engaging in multiple pathways [1] [2].

FK-739 is an angiotensin type 1 receptor antagonist. FK 739 inhibits the specific binding of [125I]-angiotensin II to rat aortic smooth muscle cell membrane (IC50 = 8.6 nM) without displacing the specific binding of [125I]-angiotensin II to bovine cerebel

PACAP (1-38) free acid TFA, an endogenous neuropeptide, effectively enhances antral motility and somatostatin secretion, while concurrently suppressing gastrin secretion and promoting the release of vasoactive intestinal polypeptide, gastrin-releasing peptide, and substance P. Additionally, it amplifies N-methyl-D-aspartate receptor function and brain-derived neurotrophic factor expression via RACK1 [1] [2].

PACAP (1-38) free acid, an endogenous neuropeptide, potently modulates gastrointestinal and neuroendocrine functions. It enhances antral motility, increases somatostatin secretion, and stimulates the release of vasoactive intestinal polypeptide, gastrin releasing peptide, and substance P, while concurrently inhibiting gastrin secretion. Additionally, it augments N-methyl-D-aspartate receptor function and upregulates brain-derived neurotrophic factor expression via RACK1 [1] [2].

EC17 is a FITC conjugated folic acid, also known as Folate-FITC. It also acts as an FRα-targeting agent that fluoresces at 500nm. EC17 is a conjugate consisting of fluorescein isothiocyanate (FITC) conjugated with folate with potential antineoplastic acti

(R)-Butaprost (free acid) is a prostaglandin E2 (PGE2) analog exhibiting high EP2 receptor subtype selectivity, commonly used to delineate EP receptor expression in human and animal tissues and cells. In 1986, Gardiner induced significant confusion regarding its structure by incorrectly identifying the selective C-16 epimer as (R)-butaprost (refer to the British Journal of Pharmacology, page 46, as TR 4979, and notes). By removing the methyl ester and restoring the native carboxylic acid at C-1, the binding affinity for prostaglandin receptors was enhanced, given such free acids typically display 10 to 100 times greater affinity than their ester counterparts. Although not extensively studied pharmacologically, (R)-butaprost is generally viewed as the less active C-16 epimer, with careful studies conducted later in the United States and Japan ultimately establishing the correct active structure as the 16(S) epimer.

Cholecystokinin (26-33) free acid, a part of cholecystokinin (CCK), is a highly selective ligand for CCKB-type receptors found in the vertebrate CNS and induces a mild taste aversion conditioned reflex in rats.

SM19712 free acid is an inhibitor of nonpeptide endothelin converting enzyme.

(S)-Butaprost (free acid) is a highly potent and selective EP2 receptor agonist[1].

Sulfazecin is a β-Lactam antibiotic.

DXR inhibitor 11a, with an IC50 of 0.11 µM, effectively inhibits P. falciparum 1-deoxy-D-xylulose-5-phosphate reductoisomerase (DXR). It also hampers the growth of P. falciparum in isolated human erythrocytes, demonstrating an IC50 of 0.37 µM.

12:0 N-Biotinyl fatty acid, a biotinylated derivative of lauric acid, serves as an intermediate for synthesizing N-biotinylated phenylarsonous acids.

Cangrelor is a P2Y12 inhibitor, and was approved in June 2015 as an antiplatelet drug for intravenous application. Cangrelor is a high-affinity, reversible inhibitor of P2Y12 receptors that causes almost complete inhibition of ADP-induced platelet aggregate. It is a modified ATP derivative stable to enzymatic degradation. It does not require metabolic conversion to an active metabolite. This allows cangrelor’s immediate effect after infusion, and the therapeutic effects can be maintained with continuous infusion.

Latanoprost is an F-series prostaglandin (PG) analog which has been approved for use as an ocular hypotensive drug. Latanoprost is an isopropyl ester, a prodrug form which is converted to latanoprost (free acid) by endogenous esterase enzymes. The free acid form is 200 times more potent than latanoprost as a ligand for the human recombinant FP receptor. 5-trans Latanoprost (free acid) is an isomer of latanoprost (free acid) wherein the double bond between carbons 5 and 6 has been changed from cis (Z) to trans (E). The trans isomer of latanoprost occurs as an impurity in commercial preparations of the bulk drug product. The present compound was prepared primarily as an analytical standard for detection and quantitation of this impurity. From what can be inferred from the study of other trans isomers of F-type prostaglandins, the biological activity of this isomer is likely to be similar to that of the cis isomer. However, there are no specific published reports on the biological activity, and on reducing intraocular pressure in particular, of 5-trans latanoprost.

Palmitic acid-13C is intended for use as an internal standard for the quantification of palmitic acid by GC- or LC-MS. Palmitic acid is a 16-carbon saturated fatty acid. It comprises approximately 25% of human total plasma lipids.1 It increases protein levels of COX-2 in RAW 264.7 cells when used at a concentration of 75 μM.2 Palmitic acid is involved in the acylation of proteins to anchor membrane-bound proteins to the lipid bilayer.2,3,4,5,6 |1. Santos, M.J., López-Jurado, M., Llopis, J., et al. Influence of dietary supplementation with fish oil on plasma fatty acid composition in coronary heart disease patients. Ann. Nutr. Metab. 39(1), 52-62 (1995).|2. Lee, J.Y., Sohn, K.H., Rhee, S.H., et al. Saturated fatty acids, but not unsaturated fatty acids, induced the expression of cyclooxygenase-2 mediated through toll-like receptor 4. J. Biol. Chem. 276(20), 16683-16689 (2001).|3. Dietzen, D.J., Hastings, W.R., and Lublin, D.M. Caveolin is palmitoylated on multiple cysteine residues. Palmitoylation is not necessary for localization of caveolin to caveolae. J. Biol. Chem. 270(12), 6838-6842 (1995).|4. Robinson, L.J., and Michel, T. Mutagenesis of palmitoylation sites in endothelial nitric oxide synthase identifies a novel motif for dual acylation and subcellular targeting. Proc. Nat. Acad. Sci. USA 92(25), 11776-11780 (1995).|5. Topinka, J.R., and Bredt, D.S. N-terminal palmitoylation of PSD-95 regulates association with cell membranes and interaction with K+ channel Kv1.4. Neuron 20(1), 125-134 (1998).|6. Miggin, S.M., Lawler, O.A., and Kinsella, B.T. Palmitoylation of the human prostacyclin receptor. Functional implications of palmitoylation and isoprenylation. J. Biol. Chem. 278(9), 6947-6958 (2003).

Palmitic acid sodium (Sodium palmitate) is a type of saturated fatty acid that is formed in fatty acid synthesis.Palmitic acid sodium promotes adipogenesis and cellular lipoatrophy in a variety of cell lines.

Palmitic acid-13C (C1, C2, C3, and C4 labeled) is intended for use as an internal standard for the quantification of palmitic acid by GC- or LC-MS. Palmitic acid is a common 16-carbon saturated fat that represents 10-20% of human dietary fat intake and comprises approximately 25 and 65% of human total plasma lipids and saturated fatty acids, respectively.1,2Acylation of palmitic acid to proteins facilitates anchoring of membrane-bound proteins to the lipid bilayer and trafficking of intracellular proteins, promotes protein-vesicle interactions, and regulates various G protein-coupled receptor functions.1Red blood cell palmitic acid levels are increased in patients with metabolic syndrome compared to patients without metabolic syndrome and are also increased in the plasma of patients with type 2 diabetes compared to individuals without diabetes.3,4 1.Fatima, S., Hu, X., Gong, R.-H., et al.Palmitic acid is an intracellular signaling molecule involved in disease developmentCell. Mol. Life Sci.76(13)2547-2557(2019) 2.Santos, M.J., López-Jurado, M., Llopis, J., et al.Influence of dietary supplementation with fish oil on plasma fatty acid composition in coronary heart disease patientsAnn. Nutr. Metab.39(1)52-62(1995) 3.Yi, L.-Z., He, J., Liang, Y.-Z., et al.Plasma fatty acid metabolic profiling and biomarkers of type 2 diabetes mellitus based on GC/MS and PLS-LDAFEBS Lett.580(30)6837-6845(2006) 4.Kabagambe, E.K., Tsai, M.Y., Hopkins, P.N., et al.Erythrocyte fatty acid composition and the metabolic syndrome: A National Heart, Lung, and Blood Institute GOLDN studyClin. Chem.54(1)154-162(2008)

Palmitic acid-13C16 sodium, a 13C-labeled form of the naturally occurring saturated fatty acid Palmitic acid sodium, is prevalent in animals and plants. This compound can trigger the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer binding protein homologous protein (CHOP) in mouse granulosa cells.

Sodium palmitate-13C is the 13C-labeled variant of palmitic acid, a long-chain saturated fatty acid prevalent in animals and plants. This compound has been shown to induce the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer-binding protein homologous protein (CHOP) in mouse granulosa cells.

Palmitic acid (Cetylic acid) is a natural product, a common saturated fatty acid found in animals, plants and microorganisms. Palmitic acid has antitumor activity.

Palmitic acid-13C2 is the 13C-labeled Palmitic acid. Palmitic acid is a long-chain saturated fatty acid commonly found in both animals and plants. Palmitic acid can induce the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer binding protein homologous protein (CHOP) in in mouse granulosa cells.