BMS-813160

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

BMS-813160是第一个进入心血管临床开发的双重CCR2/CCR5拮抗剂。

BMS-813160 is the first dual?CCR2/CCR5?antagonist to enter Clinical development for cardiovascular.(In Vitro):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.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.(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.

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.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.

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. Animal Model:Human-CCR2 knock-in C57BL/6 male mice with thioglycollate injectionDosage:10, 50 and 160 mg/kg Administration:Oral gavage; 10-160 mg/kg twice a day; for two days Result:Dose-dependently reduced inflammatory monocyte and macrophage infiltration in the peritoneum.

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Cell Cycle/DNA Damage

Potassium Channel

CCR2|CCR5

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1286279-29-5

484.64

C25H40N8O2

>98% (HPLC)

DMSO : 25 mg/mL 51.58 mM;

CC(C)(C)N[C@@H]1CC[C@@H]([C@H](NC(C)=O)C1)N4CC[C@H](Nc2ncnc3cc(nn23)C(C)(C)C)C4=O

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(-20℃)

With Ice Pack

≥ 2 years