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CAS No. : 497223-25-3
MCE 国际站:Cenicriviroc
产品活性:Cenicriviroc (TAK-652) 是一种可口服的 CCR2/CCR5 双重拮抗剂,同时可抑制 HIV-1 和 HIV-2,具有显著的抗炎、抗感染的功效。
研究领域:GPCR/G Protein | Immunology/Inflammation | Anti-infection
作用靶点:CCR | HIV
In Vitro: Cenicriviroc prevents human immunodeficiency virus type 1 (HIV-1) from cellular entry. Regarding the 4 R5 HIV-2 clinical isolates tested, effective concentration 50% EC50 for cenicriviroc are 0.03, 0.33, 0.45 and 0.98 nM. The dual-tropic and the X4-tropic HIV-2 strains are resistant to cenicriviroc with EC50 at >1000 nM, and MPI at 33% and 4%, respectively.
In Vivo: Cenicriviroc (≥20 mg/kg/day) significantly reduces monocyte/macrophage recruitment in vivo. At these doses, cenicriviroc shows antifibrotic effects, with significant reductions in collagen deposition, and collagen type 1 protein and mRNA expression across the three animal models of fibrosis. In the NASH model, cenicriviroc significantly reduces the non-alcoholic fatty liver disease activity score. Cenicriviroc treatment has no notable effect on body or liver/kidney weight.
相关产品:Drug Repurposing Compound Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | Anti-Infection Compound Library | GPCR/G Protein Compound Library | Immunology/Inflammation Compound Library | Clinical Compound Library | Antiviral Compound Library | Small Molecule Immuno-Oncology Compound Library | Drug Repurposing Compound Library | Endocrinology Compound Library | Orally Active Compound Library | Rare Diseases Drug Library | Anti-Pulmonary Fibrosis Compound Library | Chemokine Compound Library | Membrane Protein-targeted Compound Library | Membrane Receptor-targeted Compound Library | Highly Selective Inhibitors Library | Peldesine dihydrochloride | Abacavir sulfate | HIV-IN-6 | Epicoccone B | Ditiocarb | Nevirapine | DAPTA | Aloperine | Elipovimab | HIV-1 inhibitor-52 | PMEDAP | Integracin B | FNC-TP | DDX3-IN-1 | BMS-753426 | Sennoside A | CK-666 | HIV-1 inhibitor-44 | Flavopiridol | Claficapavir | Atazanavir | 1-Deoxymannojirimycin hydrochloride | TC14012 | BMS-813160 | (Z)-9-Propenyladenine | Apabetalone | JNJ-27141491 | CCR5 antagonist 2 | 2F5 epitope | HIV-1 inhibitor-23
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