Cenicriviroc|497223-25-3|(TAK-652; TBR-652)-陌孚医药/Medlife

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Cenicriviroc (Synonyms: TAK-652; TBR-652)

目录号: PL04297 纯度: ≥99%

CAS No. :497223-25-3

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中文名称	Cenicriviroc
英文名称	Cenicriviroc
英文别名	1-Benzazocine-5-carboxamide, 8-[4-(2-butoxyethoxy)phenyl]-1,2,3,4-tetrahydro-1-(2-methylpropyl)-N-[4- [(S)-[(1-propyl-1H-imidazol-5-yl)methyl]sulfinyl]phenyl]-;Cenicriviroc;1-Benzazocine-5-carboxamide, 8-[4-(2-butoxyethoxy)phenyl]-1,2,3,4-tetrahydro-1-(2-methylpropyl)-N-[4- [(S)-[(1-propyl-1H-im;1-Benzazocine-5-carboxamide,8-[4-(2-butoxyethoxy)phenyl]-1,2,3,4-tetrahydro-1-(2-methylpropyl)-N-[4-[(S)-[(1-propyl-1H-imidazol-5-yl)methyl]sulfinyl]phenyl]-;TAK652;TAK-652;TBR652;TBR-652;(-)-8-[4-(2-Butoxyethoxy)phenyl]-1-isobutyl-N-[4-[[(1-propyl-1H-imidazol-5-yl)methyl]sulfinyl]phenyl]-1,2,3,4-tetrahydro-1-benzazocine-5-carboxamide;TB 652;Tobira;TBR 652;15C116UA4Y;(S,E)-8-(4-(2-butoxyethoxy)phenyl)-1-isobutyl-N-(4-(((1-propyl-1H-imidazol-5-yl)methyl)sulfinyl)phenyl)-1,2,3,4-tetrahydrobenzo[b]azocine-5-carboxamide;TAK 652;(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;CVC;cenicrivirocum;(-)-8-(4-(2-butoxyethoxy)phenyl)-1-isobutyl-n-(4-(((1-p
Cas No.	497223-25-3
分子式	C₄₁H₅₂N₄O₄S
分子量	696.94
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

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。

生物活性

Cenicriviroc (TAK-652) is an orally active, dual CCR2/CCR5 antagonist, also inhibits both HIV-1 and HIV-2, and displays potent anti-inflammatory and antiinfective activity.

性状

Solid

IC50 & Target[1][2]

CCR5 0.29 nM (IC50) CCR2 5.9 nM (IC50

体外研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[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
[2]. Kuwata T, et al. Incompatible Natures of the HIV-1 Envelope in Resistance to the CCR5 Antagonist Cenicriviroc and to Neutralizing Antibodies. Antimicrob Agents Chemother. 2015 Nov 2;60(1):437-5

溶解度数据	In Vitro: DMSO : 50 mg/mL (71.74 mM; Need ultrasonic)H₂O : < 0.1 mg/mL (insoluble)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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