[CAS NO. 445479-97-0] BMS CCR2 22
PRODUCTS SPECIFICATIONS [445479-97-0]
DESCRIPTION [445479-97-0]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 593.66 |
| Molecular Formula | C28H34F3N5O4S |
| SMILES | 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 |
Summary
BMS CCR2 22 is a potent, specific and high affinity CC-type chemokine receptor 2 (CCR2) antagonist with excellent binding affinity (binding IC 50 of 5.1 nM) and potent functional antagonism (calcium flux IC 50 of 18 nM and chemotaxis IC 50 of 1 nM) [1] [2] .
IC50 & Target
|
CCR2 5.1 nM (IC 50 ) |
In Vitro
BMS CCR2 22 (Compound 22) has binding affinity for wild-type and E291A mutants with
IC
50
values of 7.5 nM and 3.7 nM, respectively
[1]
.
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
IC
50
value of approximately 2 nM
[2]
.
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)
[3]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 250 mg/mL ( 421.12 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.6845 mL | 8.4223 mL | 16.8447 mL |
| 5 mM | 0.3369 mL | 1.6845 mL | 3.3689 mL |
| 10 mM | 0.1684 mL | 0.8422 mL | 1.6845 mL |
-
1.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.08 mg/mL (3.50 mM); Clear solution
References
- [1] Cherney RJ, et al. Discovery of disubstituted cyclohexanes as a new class of CC chemokine receptor 2 antagonists. J Med Chem. 2008 Feb 28;51(4):721-4.
- [2] Kredel S, et al. High-content analysis of CCR2 antagonists on human primary monocytes. J Biomol Screen. 2011 Aug;16(7):683-93.
- [3] D'Antoni ML, et al. Cenicriviroc inhibits trans-endothelial passage of monocytes and is associated with impaired E-selectin expression. J Leukoc Biol. 2018 Dec;104(6):1241-1252.
Synonyms