BMS-753426 | CCR2 inhibitor | Probechem Biochemicals

Chemical Structure : BMS-753426

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BMS-753426 (BMS 753426)

货号: PC-49142Not For Human Use, Lab Use Only.

BMS-753426 is a potent, selective and orally bioavailable antagonist of CCR2 with binding IC50 of 2.7 nM, 30-fold selectivity over CCR5.

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生物&药学活性

BMS-753426 is a potent, selective and orally bioavailable antagonist of CCR2 with binding IC50 of 2.7 nM, 30-fold selectivity over CCR5.
BMS-753426 potently inhibits chemotaxis of human peripheral blood mononuclear cells (hPBMCs) induced by 10 nM MCP-1 with IC50 of 0.8 nM.
BMS-753426 (1, 25, and 100 mg/kg, oral) inhibits 28%, 74%, and 78% of monocyte/macrophage influx, respectively, in hCCR2 knock-in (KI) mice, with EC50 of 3.9 nM.
BMS-753426 (25 mg/kg, BID) reduces clinical score, histological evaluation of the spinal cordexperimental autoimmune encephalomyelitis (EAE) model of multiple sclerosis in hCCR2 KI mice.

物理化学性质&存储条件

分子量	506.574
分子式	C25H33F3N6O2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-2-oxo-3-((6-(trifluoromethyl)quinazolin-4-yl)amino)pyrrolidin-1-yl)cyclohexyl)acetamide

参考文献

1. Michael G Yang, et al. ACS Med Chem Lett. 2021 May 25;12(6):969-975.

BMS-753426 (BMS 753426)

生物&药学活性

物理化学性质&存储条件

参考文献

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BMS-753426 (BMS 753426)

生物&药学活性

物理化学性质&存储条件

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