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Cenicriviroc
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Cenicriviroc图片
CAS NO:497223-25-3
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW) 696.94
Formula C41H52N4O4S
CAS No. 497223-25-3 (free base); 497223-28-6 (mesylate);
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 10 mM
Water: < 1 mg/mL
Ethanol: < 1 mg/mL
Chemical Name(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
SynonymsTAK 652; TBR652; Cenicriviroc; TBR-652; TBR 652; TAK-652; TAK652;
实验参考方法
In Vitro

In vitro activity: Cenicriviroc (formerly known as TAK-652 or TBR-652) is a novel, orally bioactive, and dual antagonist of CCR2/CCR5, it also inhibits both HIV-1 and HIV-2, and has the potential for the treatment of HIV infection. TAK-652 inhibited the binding of RANTES (regulated on activation, normal T-cell expressed and secreted), macrophage inflammatory protein 1alpha (MIP-1alpha), and MIP-1beta to CCR5-expressing cells at nanomolar concentrations. TAK-652 could also suppress the binding of monocyte chemotactic protein 1 (MCP-1) to CCR2b-expressing cells. However, its inhibitory effect on ligand binding to other chemokine receptors was limited. TAK-652 was active against CCR5-using (R5) HIV-1 but totally inactive against CXCR4-using (X4) HIV-1.


Kinase Assay: Cenicriviroc prevents human immunodeficiency virus type 1 (HIV-1) from cellular entry with effective concentration 50% EC50 of 0.03, 0.33, 0.45 and 0.98 nM for the 4 R5 HIV-2 clinical isolates tested. 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.


Cell Assay: AK-652 inhibited the binding of RANTES (regulated on activation, normal T-cell expressed and secreted), macrophage inflammatory protein 1alpha (MIP-1alpha), and MIP-1beta to CCR5-expressing cells at nanomolar concentrations. TAK-652 could also suppress the binding of monocyte chemotactic protein 1 (MCP-1) to CCR2b-expressing cells.

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.
Animal model Male C57BL/6 mice
Formulation & Dosage 5,20,100 mg/kg/day; oral gavage
References PLoS One. 2016 Jun 27;11(6):e0158156.