BMS-22

Research use only, not for human use.

A potent, selective, allosteric CCR2 antagonist with binding IC50 of 5.1 nM.

A potent, selective, allosteric CCR2 antagonist with binding IC50 of 5.1 nM; displays potent functional antagonism (calcium flux IC50=18 nM and chemotaxis IC 50=1 nM).

BMS CCR2 22 (Compound 22) has binding affinity for wild-type and E291A mutants with IC50 values of 7.5 nM and 3.7 nM, respectively.BMS CCR2 22 prevents both the binding and the internalization of fluorescently labeled hMCP-1_AF647 internalization in human monocytes. BMS CCR2 22 inhibits the internalization of hMCP1_AF647 with an IC50 value of approximately 2 nM.The addition of BMS CCR2 22 (0.1-10 μM; 24 h), cenicriviroc (CVC) or a combination of both BMS CCR2 22 and MVC to human aortic endothelial cells (HAoECs) prior to MCP-1 stimulation do not alter E-selectin, ICAM-1, or CD99 cell surface expression. Incubation of HAoECs with BMS CCR2 22 before MCP-1 significantly increases VCAM-1 and PECAM1 cell surface levels (from 72.8 to 160% and from 97.2 and 127%, respectively).

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BMS 22 | CCR2 inhibitor BMS 22

GPCR/G Protein

Chemokine Receptor

Chemokine Receptor

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445479-97-0

593.66

C28H34F3N5O4S

>98% (HPLC)

In Vitro:?DMSO : 250 mg/mL (421.12 mM)

O=C(NCC(N[C@H]1[C@@H](NC(C2=CC=C(SC)C=C2)=O)CCCC1)=O)C3=CC(C(F)(F)F)=CC=C3NC(NC(C)C)=O

2-[(isopropylaminocarbonyl)amino]-N-[2-[[cis-2-[[4-(methylthio)benzoyl]amino]cyclohexyl]amino]-2-oxoethyl]-5-(trifluoromethyl)benzamide

(-20℃)

With Ice Pack

≥ 2 years