S88342 |
CS-2742 |
源叶(MedMol) | 98% |
- 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。
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)