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PSN 375963 hydrochloride

GPR119 receptor agonist CAS# 388575-52-8

PSN 375963 hydrochloride

Catalog No. BCC7663----Order now to get a substantial discount!

Product Name & Size Price Stock
PSN 375963 hydrochloride: 5mg $115 In Stock
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Chemical structure

PSN 375963 hydrochloride

3D structure

Chemical Properties of PSN 375963 hydrochloride

Cas No. 388575-52-8 SDF Download SDF
PubChem ID 56972228 Appearance Powder
Formula C17H24ClN3O M.Wt 321.84
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 100 mM in DMSO and to 100 mM in ethanol
Chemical Name 5-(4-butylcyclohexyl)-3-pyridin-4-yl-1,2,4-oxadiazole;hydrochloride
SMILES CCCCC1CCC(CC1)C2=NC(=NO2)C3=CC=NC=C3.Cl
Standard InChIKey ONDLSENXTCSHGC-UHFFFAOYSA-N
Standard InChI InChI=1S/C17H23N3O.ClH/c1-2-3-4-13-5-7-15(8-6-13)17-19-16(20-21-17)14-9-11-18-12-10-14;/h9-13,15H,2-8H2,1H3;1H
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of PSN 375963 hydrochloride

DescriptionGPR119 receptor agonist (EC50 values are 8.4 and 7.9 μM at human and mouse receptors respectively). Displays similar potency to the endogenous ligand oleylethanolamide (OEA).

PSN 375963 hydrochloride Dilution Calculator

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PSN 375963 hydrochloride Molarity Calculator

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Preparing Stock Solutions of PSN 375963 hydrochloride

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.1071 mL 15.5357 mL 31.0713 mL 62.1427 mL 77.6783 mL
5 mM 0.6214 mL 3.1071 mL 6.2143 mL 12.4285 mL 15.5357 mL
10 mM 0.3107 mL 1.5536 mL 3.1071 mL 6.2143 mL 7.7678 mL
50 mM 0.0621 mL 0.3107 mL 0.6214 mL 1.2429 mL 1.5536 mL
100 mM 0.0311 mL 0.1554 mL 0.3107 mL 0.6214 mL 0.7768 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on PSN 375963 hydrochloride

Endogenous and synthetic agonists of GPR119 differ in signalling pathways and their effects on insulin secretion in MIN6c4 insulinoma cells.[Pubmed:18724386]

Br J Pharmacol. 2008 Dec;155(7):1056-65.

BACKGROUND AND PURPOSE: GPR119 is a G protein-coupled receptor that is preferentially expressed in islet cells and mediates insulin secretion. Oleoyl-lysophosphatidylcholine and oleoylethanolamide (OEA) act as endogenous ligands for this receptor, whereas PSN375963 and PSN632408 are two recently reported synthetic agonists. In this study, we explored mechanisms underlying GPR119-induced insulin secretion. In addition, we assessed the potential utility of the synthetic agonists as tools for exploring GPR119 biology. EXPERIMENTAL APPROACH: We examined natural and synthetic GPR119 agonist activity at GPR119 in MIN6c4 and RINm5f insulinoma cells. We evaluated insulin secretion, intracellular calcium [Ca(2+)](i), ion channel involvement and levels of cAMP. KEY RESULTS: We report that increases in insulin secretion induced by OEA were associated with increased cAMP and a potentiation of glucose-stimulated increases in [Ca(2+)](i). We also demonstrate that ATP-sensitive K(+) and voltage-dependent calcium channels were required for GPR119-mediated increases in glucose-stimulated insulin secretion. In contrast to OEA, the synthetic GPR119 agonist PSN375963 and PSN632408 have divergent effects on insulin secretion, cAMP and intracellular calcium in MIN6c4 cells. CONCLUSIONS AND IMPLICATIONS: The endogenous ligand OEA signals through GPR119 in a manner similar to glucagon-like peptide-1 (GLP-1) and its receptor with respect to insulin secretion, [Ca(2+)](i) and cAMP. In addition, PSN375963 and PSN632408 substantially differ from OEA and from one another. These studies suggest that the commercially available synthetic agonists, although they do activate GPR119, may also activate GPR119-independent pathways and are thus unsuitable as GPR119-specific pharmacological tools.

Deorphanization of a G protein-coupled receptor for oleoylethanolamide and its use in the discovery of small-molecule hypophagic agents.[Pubmed:16517404]

Cell Metab. 2006 Mar;3(3):167-75.

The endogenous lipid signaling agent oleoylethanolamide (OEA) has recently been described as a peripherally acting agent that reduces food intake and body weight gain in rat feeding models. This paper presents evidence that OEA is an endogenous ligand of the orphan receptor GPR119, a G protein-coupled receptor (GPCR) expressed predominantly in the human and rodent pancreas and gastrointestinal tract and also in rodent brain, suggesting that the reported effects of OEA on food intake may be mediated, at least in part, via the GPR119 receptor. Furthermore, we have used the recombinant receptor to discover novel selective small-molecule GPR119 agonists, typified by PSN632408, which suppress food intake in rats and reduce body weight gain and white adipose tissue deposition upon subchronic oral administration to high-fat-fed rats. GPR119 therefore represents a novel and attractive potential target for the therapy of obesity and related metabolic disorders.

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