PSN632408

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

MedKoo CAT#: 522483

CAS#: 857652-30-3

Description: 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

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PSN632408
CAS# 857652-30-3

Theoretical Analysis

MedKoo Cat#: 522483
Name: PSN632408
CAS#: 857652-30-3
Chemical Formula: C18H24N4O4
Exact Mass: 360.17976
Molecular Weight: 360.414
Elemental Analysis: C, 59.99; H, 6.71; N, 15.55; O, 17.76

Size Price Shipping out time Quantity
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Pricing updated 2021-03-02. Prices are subject to change without notice.

PSN632408 is not in stock, may be available through custom synthesis. For cost-effective reason, minimum 1 gram order is requested. The product will be characterized by NMR, HPLC and MS analysis. Purity (HPLC) is usually >98%. CoA, QC data, MSDS will be provided when product is successfully made. The estimated lead time is 2-3 months. Please send email to sales@medkoo.com to inquire quote.

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

Handling Instructions:

Preparing Stock Solutions

The following data is based on the product molecular weight 360.414 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.

Select a batch to recalculate based on the batch molecular weight:
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

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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.