BMS-817399

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-817399 是一种有效的、选择性的、口服生物可利用的 CCR1 拮抗剂，结合 IC50 为 1 nM，抑制 MIP-1α 诱导的趋化性，IC50 为 6 nM。

BMS-817399 is a potent, selective, orally bioavailable CCR1 antagonist with binding IC50 of 1 nM, inhibits MIP-1α-induced chemotaxis with IC50 of 6 nM; shows no binding activity to other CC family receptors, including CCR2, CCR3, CCR4, CCR5, CXCR2, CXCR3, and CXCR5, as well as a broad panel of other GPCRs and biogenic amine transporters; blocks MIP1α- and LKN-1-mediated up-regulation of CD11b in human whole blood with IC50 values of 25 nM and 42 nM, respectively; shows potential for the treatment of rheumatoid arthritis.Rheumatoid Arthritis Phase 2 Discontinued.

In addition to MIP-1α (CCL3), BMS-817399 potently inhibits chemotaxis induced by other CCR1 ligands.

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BMS817399

GPCR/G Protein

Chemokine Receptor

Chemokine Receptor

Inflammation/Immunology

Rheumatoid Arthritis

1202400-18-7

454.008

C23H36ClN3O4

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (220.26 mM)

CC(C)C(C(=O)N1CCC(C(C1)(C)C)(C2=CC=C(C=C2)Cl)O)NC(=O)NCC(C)(C)O

1-((R)-1-((S)-4-(4-chlorophenyl)-4-hydroxy-3,3-dimethylpiperidin-1-yl)-3-methyl-1-oxobutan-2-yl)-3-(2-hydroxy-2-methylpropyl)urea

(-20℃)

With Ice Pack

≥ 2 years