CP-481715

Research use only, not for human use.

CP-481715 is a potent and selective CCR1 antagonist with Ki of 9.2 nM and IC50 of 74 nM.

CP-481715 is a potent and selective CCR1 antagonist with Ki of 9.2 nM and IC50 of 74 nM, lacks intrinsic agonist activity and ; displays >100-fold selectiveity over a panel of GPCRs including related chemokine receptors; fully blocks the ability of CCL3 and CCL5 to stimulate receptor signaling (calcium mobilization, IC50=71 nM), monocyte chemotaxis, IC50= 55 nM, and MMP 9 release, IC50= 54 nM); inhibits cell infiltration and inflammatory responses in human CCR1 transgenic mice.Rheumatoid Arthritis Phase 1 Discontinued.

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CP481715

GPCR/G Protein

Chemokine Receptor

Chemokine Receptor

Inflammation/Immunology

Rheumatoid Arthritis

212790-31-3

482.556

C26H31FN4O4

>98% (HPLC)

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O=C(C1=NC2=CC=CC=C2N=C1)N[C@@H](CC3=CC=CC(F)=C3)[C@@H](O)C[C@H](C(N)=O)CCC(C)(O)C

N-[(2S,3S,5R)-5-carbamoyl-1-(3-fluorophenyl)-3,8-dihydroxy-8-methylnonan-2-yl]quinoxaline-2-carboxamide

(-20℃)

With Ice Pack

≥ 2 years