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首页-小分子抑制剂&激动剂-GPCR-Chemokine Receptor (CCR and CXCR)-Cenicriviroc
Cenicriviroc

Chemical Structure : Cenicriviroc

CAS No.: 497223-25-3

Cenicriviroc (TBR-652, TAK-652)

货号: PC-38499Not For Human Use, Lab Use Only.

Cenicriviroc (TAK-652, TBR-652) is a potent, selective, orally active, dual CCR2/CCR5 antagonist with IC50 of 5.9/0.29 nM, inhibits both HIV-1 and HIV-2 and prevents viral cellular entry.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Cenicriviroc (TAK-652, TBR-652) is a potent, selective, orally active, dual CCR2/CCR5 antagonist with IC50 of 5.9/0.29 nM, inhibits both HIV-1 and HIV-2 and prevents viral cellular entry.
Cenicriviroc (TAK-652, TBR-652) exhibits effective EC50 of 0.03, 0.33, 0.45 and 0.98 nM against 4 R5 HIV-2 clinical isolates.
Cenicriviroc (≥20 mg/kg/day) significantly reduces monocyte/macrophage recruitment in vivo.
Cenicriviroc (TAK-652, TBR-652) shows antifibrotic effects, with significant reductions in collagen deposition, and collagen type 1 protein and mRNA expression across animal models of fibrosis.

物理化学性质&存储条件

分子量 696.94
分子式 C41H52N4O4S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(5E)-8-[4-(2-butoxyethoxy)phenyl]-1-(2-methylpropyl)-N-[4-[(S)-(3-propylimidazol-4-yl)methylsulfinyl]phenyl]-3,4-dihydro-2H-1-benzazocine-5-carboxamide

参考文献

1. Lefebvre E, et al. PLoS One. 2016 Jun 27;11(6):e0158156

2. Kuwata T, et al. Antimicrob Agents Chemother. 2015 Nov 2;60(1):437-5

3. Baba M, et al. Antimicrob Agents Chemother. 2005 Nov;49(11):4584-91.

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