化合物Cenicriviroc TQ0297

Product Introduction
Bioactivity


英文名: Cenicriviroc

描述: Cenicriviroc (TAK-652) 是一种可口服的CCR2/CCR5拮抗剂，可抑制 HIV-1 和 HIV-2，具有抗炎、抗感染作用。

动物实验: Male C57BL/6 mice (n=44; 8-10 weeks of age) are allocated to receive treatments via oral gavage (PO) on Days 1-5 in the following groups: non-disease control, vehicle control twice daily (BID), Cenicriviroc 5 mg/kg/day (Cenicriviroc5) BID, Cenicriviroc 20 mg/kg/day (Cenicriviroc20) BID, Cenicriviroc 100 mg/kg/day (Cenicriviroc100) BID, Cenicriviroc20 QD, and positive control (corticosteroid known to reduce inflammation in a variety of animal models) 1 mg/kg QD. On Day 4, peritonitis is induced via IP injection of TG 3.85% (1 mL/animal) 2 hours post-dose in all groups except non-disease controls [1].

体外活性: Cenicriviroc 阻止 HIV-1 的细胞进入[2]。就测试的 4 个 R5 HIV-2 临床分离株而言，cenicriviroc 的有效浓度 50% (EC50) 分别为 0.03、0.33、0.45 和 0.98 nM。具有双重亲和性和 X4-亲和性的 HIV-2 株对 cenicriviroc 显示出抗性，其 EC50 值均 >1000 nM，MPI 分别为 33% 和 4% [3]。

体内活性: Cenicriviroc (≥20 mg/kg/天) 在体内显著减少单核细胞/巨噬细胞的招募。在NASH模型中，cenicriviroc 显著降低非酒精性脂肪肝病活动评分。Cenicriviroc治疗对体重或肝/肾重量没有显著影响[1]。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 120 mg/mL (172.19 mM)


关键字: CC chemokine receptor | Cenicriviroc | inhibit | HIV | TAK652 | Inhibitor | Human immunodeficiency virus | TAK 652 | TBR652 | TBR 652 | CCR

相关产品: Emivirine | FGI-106 tetrahydrochloride | Atazanavir sulfate | Plerixafor octahydrochloride | Valproic acid sodium salt | Peldesine | Oleanonic acid | 3',5,5',7-Tetrahydroxy-4',6-dimethoxyflavone | HIV-1 Rev (34-50) | Tenofovir

相关库: Drug Repurposing Compound Library | Cytokine Inhibitor Library | Immuno-Oncology Compound Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Chemokine Inhibitor Library | Orally Active Compound Library | NO PAINS Compound Library | Anti-Viral Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途