| 产品描述: | BMS-813160 is a potent and selective CCR2/5 dual antagonist. BMS-813160 binds with CCR2 and CCR5 with IC50s of 6.2 and 3.6 nM, respectively. BMS-813160 can be used for the research of inflammation |
| 靶点: |
CCR5:3.6 nM (IC50);CCR2:6.2 nM (IC50);CCR |
| 体外研究: |
BMS-813160 binds with CCR2, CCR5, CCR1, CCR4 and CXCR2 with IC50s of 6.2 nM, 3.6 nM, >25 μM, >40 μM and >40 μM, respectively. BMS-813160 shows activities to CCR2 CTX, CCR2 CD11b, CCR5 CTX and CCR5 CD11b with IC50s of 0.8, 4.8, 1.1 and 5.7 nM, respectively |
| 体内研究: |
BMS-813160 (10-160 mg/kg; p.o. twice a day for two days) inhibits the migration of inflammatory monocytes and macrophages in mouse thioglycollate-induced peritonitis model, and shows excellent oral bioavailability. Animal Model: Human-CCR2 knock-in C57BL/6 male mice with thioglycollate injection Dosage: 10, 50 and 160 mg/kg Administration: Oral gavage; 10-160 mg/kg twice a day; for two days Result: Dose-dependently reduced inflammatory monocyte and macrophage infiltration in the peritoneum. |
| 参考文献: |
1. Norman P. et al. A dual CCR2/CCR5 chemokine antagonist, BMS-813160? Evaluation of WO2011046916. Expert Opin Ther Pat. 2011 Dec;21(12):1919-24. 2. Cherney RJ, et al. BMS-813160: A Potent CCR2 and CCR5 Dual Antagonist Selected as a Clinical Candidate. ACS Med Chem Lett. 2021 Oct 15;12(11):1753-1758. |
| 溶解性: |
Soluble in DMSO |
| 保存条件: |
2-8°C |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.063 ml |
10.317 ml |
20.634 ml |
| 5 mM |
0.413 ml |
2.063 ml |
4.127 ml |
| 10 mM |
0.206 ml |
1.032 ml |
2.063 ml |
| 50 mM |
0.041 ml |
0.206 ml |
0.413 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |