Cenicriviroc Mesylate
(Synonyms: TAK-652 Mesylate; TBR-652 Mesylate) 目录号 : GC35650
An antagonist of CCR5 and CCR2
Cas No.:497223-28-6
Sample solution is provided at 25 µL, 10mM.
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Cenicriviroc is an orally bioavailable antagonist of C-C chemokine receptor type 5 (CCR5) and CCR2 that inhibits binding of macrophage inflammatory protein 1α (MIP-1α; IC50 = 2.3 nM) and monocyte chemotactic protein 1 (MCP-1; IC50 = 5.9 nM), respectively, in CHO cells.1 Cenicriviroc is also an antagonist of CCR3 and CCR4 (IC50s = 2.4 and 1.1 μM, respectively), however, it does not inhibit agonist binding to CCR1 or CCR7 at concentrations up to 10 μM. At a concentration of 100 nM, cenicriviroc completely inhibits replication of R5 HIV-1 in U87.CD4.CCR5 cells. Cenicriviroc inhibits replication of the R5 HIV-1 strains JR-FL and KK in peripheral blood mononuclear cells (PBMCs) with EC50 values ranging from 21 to 210 pM and 33 to 91 pM, respectively. In vivo, cenicriviroc (20 mg/kg per day) reduces collagen deposition, levels of collagen type 1 protein and mRNA expression, and non-alcoholic fatty liver disease activity score in a mouse model of non-alcoholic steatohepatitis (NASH).2 It also reduces collagen type 1 protein levels, mRNA expression, and collagen deposition in a mouse model of unilateral ureter obstruction and a rat model of thioacetamide-induced liver fibrosis.
1.Baba, M., Takashima, K., Miyake, H., et al.TAK-652 inhibits CCR5-mediated human immunodeficiency virus type 1 infection in vitro and has favorable pharmacokinetics in humansAntimicrob. Agents Chemother.49(11)4584-4591(2005) 2.Lefebvre, E., Moyle, G., Reshef, R., et al.Antifibrotic effects of the dual CCR2/CCR5 antagonist cenicriviroc in animal models of liver and kidney fibrosisPLoS One11(6):e0158156(2016)
Cell experiment: | Mouse monocyte migration in response to Cenicriviroc Mesylate (CVC) treatment is assessed ex vivo in triplicate. Thioglycollate (TG) is injected intraperitoneally into male C57BL/6 mice (n=3; 8 to 10 weeks of age) and activated macrophages are collected 48 hours later by peritoneal lavage. Cells are incubated for 2 hours in the presence of 1 μM Cenicriviroc Mesylate. Cells are harvested from the lower compartment and analyzed by flow cytometry to enumerate F4/80+CD11b+ macrophages. Results are analyzed using FlowJo software[1]. |
Animal experiment: | Male C57BL/6 mice (n=44; 8 to 10 weeks of age) are allocated to receive treatments via oral gavage (PO) on Days 1 to 5 in the following groups: non-disease control, vehicle control twice daily (BID), Cenicriviroc Mesylate 5 mg/kg/day (CVC5) BID, Cenicriviroc Mesylate 20 mg/kg/day (CVC20) BID, Cenicriviroc Mesylate 100 mg/kg/day (CVC100) BID, Cenicriviroc Mesylate 20 mg/kg once-daily (QD). On Day 4, peritonitis is induced via IP injection of thioglycollate (TG) 3.85% (1 mL/animal) 2 hours post-dose in all groups except non-disease controls[1]. |
References: [1]. Lefebvre E, et al. Antifibrotic Effects of the Dual CCR2/CCR5 Antagonist Cenicriviroc in Animal Models of Liver and Kidney Fibrosis. PLoS One. 2016 Jun 27;11(6):e0158156. | |
| Cas No. | 497223-28-6 | SDF | |
| 别名 | TAK-652 Mesylate; TBR-652 Mesylate | ||
| Canonical SMILES | O=C(/C1=C/C2=CC(C3=CC=C(OCCOCCCC)C=C3)=CC=C2N(CC(C)C)CCC1)NC4=CC=C([S@](CC5=CN=CN5CCC)=O)C=C4.OS(=O)(C)=O | ||
| 分子式 | C42H56N4O7S2 | 分子量 | 793.05 |
| 溶解度 | DMSO: 100 mg/mL (126.10 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.261 mL | 6.3048 mL | 12.6095 mL |
| 5 mM | 0.2522 mL | 1.261 mL | 2.5219 mL |
| 10 mM | 0.1261 mL | 0.6305 mL | 1.261 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet