BMS-813160_product_DataBase

Bioactivity	BMS-813160 is a potent and selective CCR2/5 dual antagonist. BMS-813160 binds with CCR2 and CCR5 with IC50s of 6.2 and 3.6 nM, respectively. BMS-813160 can be used for the research of inflammation[1][2].
Invitro	BMS-813160 binds with CCR2, CCR5, CCR1, CCR4 and CXCR2 with IC50s of 6.2 nM, 3.6 nM, ＞25 μM, ＞40 μM and ＞40 μM, respectively[2]. BMS-813160 shows activities to CCR2 CTX, CCR2 CD11b, CCR5 CTX and CCR5 CD11b with IC50s of 0.8, 4.8, 1.1 and 5.7 nM, respectively[2].
In Vivo	BMS-813160 (10-160 mg/kg; p.o. twice a day for two days) inhibits the migration of inflammatory monocytes and macrophages in mouse thioglycollate-induced peritonitis model, and shows excellent oral bioavailability[2]. Animal Model:
Name	BMS-813160
CAS	1286279-29-5
Formula	C25H40N8O2
Molar Mass	484.64
Appearance	Solid
Transport	Room temperature in continental US; may vary elsewhere.
Storage	4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Reference	[1]. Norman P. et al. A dual CCR2/CCR5 chemokine antagonist, BMS-813160? Evaluation of WO2011046916. Expert Opin Ther Pat. 2011 Dec;21(12):1919-24. [2]. Cherney RJ, et al. BMS-813160: A Potent CCR2 and CCR5 Dual Antagonist Selected as a Clinical Candidate. ACS Med Chem Lett. 2021 Oct 15;12(11):1753-1758.

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