BMS-817399( BMS817399 )

Catalog No. M10732 CAS No. 1202400-18-7

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

BMS-817399
Note

Research use only, not for human use.
Brief Description

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.
Description

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 Vitro

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

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Synonyms

BMS817399
Pathway

GPCR/G Protein
Target

Chemokine Receptor
Recptor

Chemokine Receptor
Research Area

Inflammation/Immunology
Indication

Rheumatoid Arthritis

CAS Number

1202400-18-7
Formula Weight

454.008
Molecular Formula

C23H36ClN3O4
Purity

>98% (HPLC)
Solubility

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

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

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

1. Santella JB 3rd, et al. J Med Chem. 2014 Sep 25;57(18):7550-64.

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