BMS-813160
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.
Product Specifications
CAS Number
1286279-29-5
Purity
>98% (HPLC)
Solubility
DMSO : 25 mg/mL 51.58 mM
Smiles
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
Molecular Formula
C25H40N8O2
Molecular Weight
484.64
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
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