AMG-131 besylate

• CAT Number: I021958
• CAS Number: 849738-78-9
• Molecular Formula: C27H18Cl4N2O6S2
• Molecular Weight: 672.37
• Purity: 98%
• Synonyms: AMG-131 besylate; AMG 131 besylate; AMG131 besylate; INT 131 besylate; INT131 besylate; INT-131 besylate
• Solubility: To be determined
• Appearance: Solid powder
• Storage: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
• IUPAC Name: benzenesulfonic acid;2,4-dichloro-N-(3,5-dichloro-4-quinolin-3-yloxyphenyl)benzenesulfonamide
• InChI: 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)
• InChIKey: ADMLKETZLUWHLX-UHFFFAOYSA-N
• SMILES: C1=CC=C(C=C1)S(=O)(=O)O.C1=CC=C2C(=C1)C=C(C=N2)OC3=C(C=C(C=C3Cl)NS(=O)(=O)C4=C(C=C(C=C4)Cl)Cl)Cl

AMG-131 besylate（Cat No.:I021958）is a novel, investigational peptide-based drug developed by Amgen, designed to target the NKG2D receptor, which plays a key role in immune system activation. The compound works by modulating the immune response, particularly in the context of cancer. NKG2D is involved in recognizing stressed or tumor cells, and AMG-131 aims to enhance this recognition, potentially boosting anti-tumor immunity. It is being evaluated in clinical trials for its potential as a cancer immunotherapy, particularly for cancers resistant to conventional treatments. Its safety and efficacy are still under investigation.

Reference

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.