PSN632408 | CAS#857652-30-3 | agonist of GPR119

MedKoo Cat#: 522483 | Name: PSN632408

Description:

WARNING: This product is for research use only, not for human or veterinary use.

PSN632408 is a potent and selective agonist of GPR119 receptors that shows similar potency to OEA at both recombinant mouse and human GPR119 receptors, exhibiting EC50 values of 5.6 and 7.9 µM, respectively (EC50 values for OEA are 3.2 and 2.9 µM, respectively). OEA and PSN632408 can stimulate β-cell replication in vitro and in vivo and improve islet graft function. PSN632408 is potential useful for treatment of diabetics.

Chemical Structure

PSN632408

CAS#857652-30-3

Theoretical Analysis

MedKoo Cat#: 522483

Name: PSN632408

CAS#: 857652-30-3

Chemical Formula: C18H24N4O4

Exact Mass: 360.1798

Molecular Weight: 360.41

Elemental Analysis: C, 59.99; H, 6.71; N, 15.55; O, 17.76

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.

Bulk Inquiry

Related CAS #

No Data

Synonym

PSN632408; PSN 632408; PSN-632408.

IUPAC/Chemical Name

tert-butyl 4-((3-(pyridin-4-yl)-1,2,4-oxadiazol-5-yl)methoxy)piperidine-1-carboxylate

InChi Key

LHZWKWCEAXQUMX-UHFFFAOYSA-N

InChi Code

InChI=1S/C18H24N4O4/c1-18(2,3)25-17(23)22-10-6-14(7-11-22)24-12-15-20-16(21-26-15)13-4-8-19-9-5-13/h4-5,8-9,14H,6-7,10-12H2,1-3H3

SMILES Code

O=C(N1CCC(OCC2=NC(C3=CC=NC=C3)=NO2)CC1)OC(C)(C)C

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO, not in water

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 360.41 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

1: Cornall LM, Hryciw DH, Mathai ML, McAinch AJ. Direct activation of the proposed anti-diabetic receptor, GPR119 in cardiomyoblasts decreases markers of muscle metabolic activity. Mol Cell Endocrinol. 2015 Feb 15;402:72-85. doi: 10.1016/j.mce.2015.01.006. Epub 2015 Jan 8. PubMed PMID: 25578601. 2: Panaro BL, Tough IR, Engelstoft MS, Matthews RT, Digby GJ, Møller CL, Svendsen B, Gribble F, Reimann F, Holst JJ, Holst B, Schwartz TW, Cox HM, Cone RD. The melanocortin-4 receptor is expressed in enteroendocrine L cells and regulates the release of peptide YY and glucagon-like peptide 1 in vivo. Cell Metab. 2014 Dec 2;20(6):1018-29. doi: 10.1016/j.cmet.2014.10.004. Epub 2014 Nov 20. PubMed PMID: 25453189; PubMed Central PMCID: PMC4255280. 3: Ansarullah, Lu Y, Holstein M, DeRuyter B, Rabinovitch A, Guo Z. Stimulating β-cell regeneration by combining a GPR119 agonist with a DPP-IV inhibitor. PLoS One. 2013;8(1):e53345. doi: 10.1371/journal.pone.0053345. Epub 2013 Jan 29. PubMed PMID: 23382843; PubMed Central PMCID: PMC3558424. 4: Cornall LM, Mathai ML, Hryciw DH, Simcocks AC, O'Brien PE, Wentworth JM, McAinch AJ. GPR119 regulates genetic markers of fatty acid oxidation in cultured skeletal muscle myotubes. Mol Cell Endocrinol. 2013 Jan 5;365(1):108-18. doi: 10.1016/j.mce.2012.10.003. Epub 2012 Oct 13. PubMed PMID: 23069642. 5: Gao J, Tian L, Weng G, Bhagroo NV, Sorenson RL, O'Brien TD, Luo J, Guo Z. Stimulating beta cell replication and improving islet graft function by GPR119 agonists. Transpl Int. 2011 Nov;24(11):1124-34. doi: 10.1111/j.1432-2277.2011.01332.x. Epub 2011 Sep 8. PubMed PMID: 21902730. 6: Cox HM, Tough IR, Woolston AM, Zhang L, Nguyen AD, Sainsbury A, Herzog H. Peptide YY is critical for acylethanolamine receptor Gpr119-induced activation of gastrointestinal mucosal responses. Cell Metab. 2010 Jun 9;11(6):532-42. doi: 10.1016/j.cmet.2010.04.014. PubMed PMID: 20519124; PubMed Central PMCID: PMC2890049. 7: Ning Y, O'Neill K, Lan H, Pang L, Shan LX, Hawes BE, Hedrick JA. Endogenous and synthetic agonists of GPR119 differ in signalling pathways and their effects on insulin secretion in MIN6c4 insulinoma cells. Br J Pharmacol. 2008 Dec;155(7):1056-65. doi: 10.1038/bjp.2008.337. Epub 2008 Aug 25. PubMed PMID: 18724386; PubMed Central PMCID: PMC2528830. 8: Overton HA, Babbs AJ, Doel SM, Fyfe MC, Gardner LS, Griffin G, Jackson HC, Procter MJ, Rasamison CM, Tang-Christensen M, Widdowson PS, Williams GM, Reynet C. Deorphanization of a G protein-coupled receptor for oleoylethanolamide and its use in the discovery of small-molecule hypophagic agents. Cell Metab. 2006 Mar;3(3):167-75. PubMed PMID: 16517404.