AMG-131 besylate | hypoglycemic agent | CAS#849738-78-9

MedKoo Cat#: 125522 | Name: AMG-131 besylate

Description:

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

AMG-131 is a hypoglycemic agent. It is a potent PPARγ partial agonist that displays robust glucose-lowering activity in rodent models of diabetes while exhibiting a reduced side-effects profile compared to marketed TZDs.

Chemical Structure

AMG-131 besylate

CAS#849738-78-9 (besylate)

Theoretical Analysis

MedKoo Cat#: 125522

Name: AMG-131 besylate

CAS#: 849738-78-9 (besylate)

Chemical Formula: C27H18Cl4N2O6S2

Exact Mass: 669.9400

Molecular Weight: 672.37

Elemental Analysis: C, 48.23; H, 2.70; Cl, 21.09; N, 4.17; O, 14.28; S, 9.54

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 #

849738-78-9 (besylate) 315224-26-1 (free base)

Synonym

AMG-131 besylate; AMG131 besylate; AMG 131 besylate; T0903131 Besylate; T 0903131 Besylate; T-0903131 Besylate; O591H1M24D; Ibrigampar Besylate; CHS-131 besylate; INT-131 besylate; INT 131 besylate; INT131 besylate;

IUPAC/Chemical Name

2,4-dichloro-N-(3,5-dichloro-4-(quinolin-3-yloxy)phenyl)benzenesulfonamide benzenesulfonate

InChi Key

ADMLKETZLUWHLX-UHFFFAOYSA-N

InChi Code

InChI=1S/C21H12Cl4N2O3S.C6H6O3S/c22-13-5-6-20(16(23)8-13)31(28,29)27-14-9-17(24)21(18(25)10-14)30-15-7-12-3-1-2-4-19(12)26-11-15;7-10(8,9)6-4-2-1-3-5-6/h1-11,27H;1-5H,(H,7,8,9)

SMILES Code

OS(=O)(=O)C1=CC=CC=C1.ClC2=CC=C(C(Cl)=C2)S(=O)(=O)NC3=CC(Cl)=C(OC4=CC5=CC=CC=C5N=C4)C(Cl)=C3

Appearance

To be determined

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

To be determined

Shelf Life

>2 years if stored properly

Drug Formulation

To be determined

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 672.37 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: DePaoli AM, Higgins LS, Henry RR, Mantzoros C, Dunn FL; INT131-007 Study Group. Can a selective PPARγ modulator improve glycemic control in patients with type 2 diabetes with fewer side effects compared with pioglitazone? Diabetes Care. 2014 Jul;37(7):1918-23. doi: 10.2337/dc13-2480. Epub 2014 Apr 10. PubMed PMID: 24722496. 2: Sahebkar A, Chew GT, Watts GF. New peroxisome proliferator-activated receptor agonists: potential treatments for atherogenic dyslipidemia and non-alcoholic fatty liver disease. Expert Opin Pharmacother. 2014 Mar;15(4):493-503. doi: 10.1517/14656566.2014.876992. Epub 2014 Jan 16. Review. PubMed PMID: 24428677. 3: Taygerly JP, McGee LR, Rubenstein SM, Houze JB, Cushing TD, Li Y, Motani A, Chen JL, Frankmoelle W, Ye G, Learned MR, Jaen J, Miao S, Timmermans PB, Thoolen M, Kearney P, Flygare J, Beckmann H, Weiszmann J, Lindstrom M, Walker N, Liu J, Biermann D, Wang Z, Hagiwara A, Iida T, Aramaki H, Kitao Y, Shinkai H, Furukawa N, Nishiu J, Nakamura M. Discovery of INT131: a selective PPARγ modulator that enhances insulin sensitivity. Bioorg Med Chem. 2013 Feb 15;21(4):979-92. doi: 10.1016/j.bmc.2012.11.058. Epub 2012 Dec 10. PubMed PMID: 23294830. 4: Lee DH, Huang H, Choi K, Mantzoros C, Kim YB. Selective PPARγ modulator INT131 normalizes insulin signaling defects and improves bone mass in diet-induced obese mice. Am J Physiol Endocrinol Metab. 2012 Mar 1;302(5):E552-60. doi: 10.1152/ajpendo.00569.2011. Epub 2012 Jan 3. PubMed PMID: 22215652; PubMed Central PMCID: PMC4116349. 5: Yew T, Toh SA, Millar JS. Selective peroxisome proliferator-activated receptor-γ modulation to reduce cardiovascular risk in patients with insulin resistance. Recent Pat Cardiovasc Drug Discov. 2012 Apr;7(1):33-41. Review. PubMed PMID: 22044303. 6: Croasdell G. American Diabetes Association--70th scientific sessions--research on novel therapeutics: part 1. IDrugs. 2010 Sep;13(9):595-7. PubMed PMID: 20799136. 7: Dunn FL, Higgins LS, Fredrickson J, DePaoli AM; INT131-004 study group. Selective modulation of PPARγ activity can lower plasma glucose without typical thiazolidinedione side-effects in patients with Type 2 diabetes. J Diabetes Complications. 2011 May-Jun;25(3):151-8. doi: 10.1016/j.jdiacomp.2010.06.006. Epub 2010 Aug 23. PubMed PMID: 20739195. 8: Higgins LS, Depaoli AM. Selective peroxisome proliferator-activated receptor gamma (PPARgamma) modulation as a strategy for safer therapeutic PPARgamma activation. Am J Clin Nutr. 2010 Jan;91(1):267S-272S. doi: 10.3945/ajcn.2009.28449E. Epub 2009 Nov 11. Review. PubMed PMID: 19906796. 9: Kim MK, Chae YN, Kim HS, Choi SH, Son MH, Kim SH, Kim JK, Moon HS, Park SK, Shin YA, Kim JG, Lee CH, Lim JI, Shin CY. PAR-1622 is a selective peroxisome proliferator-activated receptor gamma partial activator with preserved antidiabetic efficacy and broader safety profile for fluid retention. Arch Pharm Res. 2009 May;32(5):721-7. doi: 10.1007/s12272-009-1511-8. Epub 2009 May 27. PubMed PMID: 19471887. 10: Motani A, Wang Z, Weiszmann J, McGee LR, Lee G, Liu Q, Staunton J, Fang Z, Fuentes H, Lindstrom M, Liu J, Biermann DH, Jaen J, Walker NP, Learned RM, Chen JL, Li Y. INT131: a selective modulator of PPAR gamma. J Mol Biol. 2009 Mar 13;386(5):1301-11. PubMed PMID: 19452630. 11: Kintscher U, Goebel M. INT-131, a PPARgamma agonist for the treatment of type 2 diabetes. Curr Opin Investig Drugs. 2009 Apr;10(4):381-7. Review. PubMed PMID: 19337960.