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

PSN632408

CAS# 857652-30-3

Instruction

Theoretical Analysis

MedKoo Cat#: 522483
Name: PSN632408
CAS#: 857652-30-3
Chemical Formula: C18H24N4O4
Exact Mass: 360.18
Molecular Weight: 360.414
Elemental Analysis: C, 59.99; H, 6.71; N, 15.55; O, 17.76

Price and Availability

Size	Price	Availability	Quantity
1g	USD -1
2g	USD -1
5g	USD -1
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

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:

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Biological target:
In vitro activity:
In vivo activity:

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

Formulation protocol:
In vitro protocol:
In vivo protocol:

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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.

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