GSK-1292263 | CAS#1032823-75-8 | GPR119 agonis

GSK-1292263
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 500890

CAS#: 1032823-75-8 (free base)

Description: GSK-1292263 is a novel GPR119 agonist that is currently under development for the treatment of type 2 diabetes. GSK1292263 improves glucose regulation in animal models of diabetes, but has no effect on plasma glucose in type 2 diabetics. Unexpectedly, GSK1292263 lowered fasting LDLc and triglycerides (TG), while increasing HDLc in the diabetic subjects. GSK1292263 has significant effects on plasma lipids and lipoprotein particles in dyslipidemic patients when dosed alone and with atorvastatin.

Chemical Structure

GSK-1292263

CAS# 1032823-75-8 (free base)

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 500890
Name: GSK-1292263
CAS#: 1032823-75-8 (free base)
Chemical Formula: C23H28N4O4S
Exact Mass: 456.18
Molecular Weight: 456.561
Elemental Analysis: C, 60.51; H, 6.18; N, 12.27; O, 14.02; S, 7.02

Price and Availability

Size	Price	Availability
10mg	USD 150
25mg	USD 250
50mg	USD 450
100mg	USD 750	2 Weeks
200mg	USD 1250	2 Weeks
500mg	USD 2450	2 Weeks
1g	USD 3450	2 Weeks
2g	USD 5650	2 Weeks
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.

Related CAS #: 1032823-75-8 (free base) 1032824-54-6 (HCl)

Synonym: GSK1292263; GSK 1292263l; GSK-1292263

IUPAC/Chemical Name: 3-isopropyl-5-(4-(((6-(4-(methylsulfonyl)phenyl)pyridin-3-yl)oxy)methyl)piperidin-1-yl)-1,2,4-oxadiazole

InChi Key: AYJRTVVIBJSSKN-UHFFFAOYSA-N

InChi Code: InChI=1S/C23H28N4O4S/c1-16(2)22-25-23(31-26-22)27-12-10-17(11-13-27)15-30-19-6-9-21(24-14-19)18-4-7-20(8-5-18)32(3,28)29/h4-9,14,16-17H,10-13,15H2,1-3H3

SMILES Code: O=S(C1=CC=C(C2=CC=C(OCC3CCN(C4=NC(C(C)C)=NO4)CC3)C=N2)C=C1)(C)=O

Appearance: Solid powder

Purity: >98%

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: >5 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: The safety, tolerability, pharmacokinetics and pharmacodynamics of single and multiple oral doses of GSK-1292263 were evaluated in a recently completed randomized, placebo-controlled clinical trial in healthy volunteers (ClinicalTrials.gov Identifier NCT00783549). A total of 69 subjects received single escalating doses of GSK-1292263 (10-400 mg) prior to administration of a 250-mg dose given once daily for 2 and 5 days, which was also evaluated in combination with sitagliptin (100 mg). Treatment with GSK-1292263 at all doses was described as well tolerated, with the most common drug-related effects being mild headache, dizziness, hyperhidrosis, flushing and post-OGTT hypoglycemia. Hypoglycemia was not reported with the 5-day dosing schedule. Pharmacokinetic profiling revealed dose-proportional AUC and Cmax at single lower doses, but not at single higher ones. Following repeated once-daily dosing (5 days), drug accumulation was observed consistent with a mean half-life of 12-18 hours. A dose-dependent increase in glucose AUC(0-3 h) during OGTT was seen in GSK-1292263-treated subjects. The treatment was also associated with an increase in PYY during the prandial periods. Coadministration with sitagliptin led to increases in the plasma concentrations of active GLP-1 but reduced the levels of total GLP-1, GIP and PYY. Sitagliptin affected the exposure to GSK-1292263 (50% increase) but GSK-1292263 did not affect sitagliptin exposure. The data support further evaluation of GSK-1292263 for the treatment of type 2 diabetes (Source: Nunez, D.J. et al. Diabetes [70th Annu Meet Sci Sess Am Diabetes Assoc (ADA) (June 25-29, Orlando) 2010] 2010, 59(Suppl. 1): Abst 80-OR).

Product Data:

Product Data

Instruction:

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Biological target:	GSK-1292263 is an orally available GPR119 agonist with pEC50s of 6.9 and 6.7 for human and rat GPR119, respectively.
In vitro activity:	Another GPR119 agonist used in clinical trials, GSK1292263, also potentiated the anti-proliferative effect of gefitinib on MCF-7 and MDA-MB-231 cells (Additional file 1: Figure S1A and B). Reference: J Exp Clin Cancer Res. 2018 Nov 29;37(1):295. https://pubmed.ncbi.nlm.nih.gov/30497501/
In vivo activity:	TBD

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	28.0	61.33

Preparing Stock Solutions

The following data is based on the product molecular weight 456.56 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:	1. Im JH, Kang KW, Kim SY, Kim YG, An YJ, Park S, Jeong BH, Choi SY, Lee JS, Kang KW. GPR119 agonist enhances gefitinib responsiveness through lactate-mediated inhibition of autophagy. J Exp Clin Cancer Res. 2018 Nov 29;37(1):295. doi: 10.1186/s13046-018-0949-2. Erratum in: J Exp Clin Cancer Res. 2022 May 17;41(1):176. PMID: 30497501; PMCID: PMC6267899.
In vitro protocol:	1. Im JH, Kang KW, Kim SY, Kim YG, An YJ, Park S, Jeong BH, Choi SY, Lee JS, Kang KW. GPR119 agonist enhances gefitinib responsiveness through lactate-mediated inhibition of autophagy. J Exp Clin Cancer Res. 2018 Nov 29;37(1):295. doi: 10.1186/s13046-018-0949-2. Erratum in: J Exp Clin Cancer Res. 2022 May 17;41(1):176. PMID: 30497501; PMCID: PMC6267899.
In vivo protocol:	TBD

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1: Yang JW, Kim HS, Im JH, Kim JW, Jun DW, Lim SC, Lee K, Choi JM, Kim SK, Kang KW. GPR119: a promising target for nonalcoholic fatty liver disease. FASEB J. 2015 Sep 23. pii: fj.15-273771. [Epub ahead of print] PubMed PMID: 26399788.

2: Nunez DJ, Bush MA, Collins DA, McMullen SL, Gillmor D, Apseloff G, Atiee G, Corsino L, Morrow L, Feldman PL. Gut hormone pharmacology of a novel GPR119 agonist (GSK1292263), metformin, and sitagliptin in type 2 diabetes mellitus: results from two randomized studies. PLoS One. 2014 Apr 3;9(4):e92494. doi: 10.1371/journal.pone.0092494. eCollection 2014. PubMed PMID: 24699248; PubMed Central PMCID: PMC3974707.

3: Kang SU. GPR119 agonists: a promising approach for T2DM treatment? A SWOT analysis of GPR119. Drug Discov Today. 2013 Dec;18(23-24):1309-15. doi: 10.1016/j.drudis.2013.09.011. Epub 2013 Sep 20. Review. PubMed PMID: 24060477.

4: Polli JW, Hussey E, Bush M, Generaux G, Smith G, Collins D, McMullen S, Turner N, Nunez DJ. Evaluation of drug interactions of GSK1292263 (a GPR119 agonist) with statins: from in vitro data to clinical study design. Xenobiotica. 2013 Jun;43(6):498-508. doi: 10.3109/00498254.2012.739719. Epub 2012 Dec 21. PubMed PMID: 23256625.

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