BMS CCR2 22 is a potent, specific and high affinity CC-type chemokine receptor 2 (CCR2) antagonist. It has excellent binding affinity (binding IC50 of 5.1 nM) and potent functional antagonism (calcium flux IC50 of 18 nM and chemotaxis IC50 of 1 nM).
| Pack Size | Availability | Price/USD | Quantity |
|---|---|---|---|
| 1 mg | 6-8 weeks | $ 161 | |
| 2 mg | 6-8 weeks | $ 273 | |
| 4 mg | 6-8 weeks | $ 462 | |
| 10 mg | 6-8 weeks | $ 961 | |
| 20 mg | 6-8 weeks | $ 1518 |
| Description | BMS CCR2 22 is a potent, specific and high affinity CC-type chemokine receptor 2 (CCR2) antagonist. It has excellent binding affinity (binding IC50 of 5.1 nM) and potent functional antagonism (calcium flux IC50 of 18 nM and chemotaxis IC50 of 1 nM). |
| Targets&IC50 | CCR2:5.1 nM |
| In vitro | BMS CCR2 22 is a potent, specific and high affinity CC-type chemokine receptor 2 (CCR2) antagonist. 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. It has excellent binding affinity (binding IC50 of 5.1 nM) and potent functional antagonism (calcium flux IC50 of 18 nM and chemotaxis IC50 of 1 nM). BMS CCR2 22 inhibits the internalization of hMCP1_AF647 with an IC50 value of approximately 2 nM. BMS CCR2 22 prevents both the binding and the internalization of fluorescently labeled hMCP-1_AF647 internalization in human monocytes. 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). |
| CAS No. | 445479-97-0 |
| Chemical Formula | C28H34F3N5O4S |
| Molecular Weight | 593.67 |
| Storage | Powder: -20°C for 2 years In solvent: -80°C for 1 year |
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