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Cenicriviroc

  Cat. No.:  DC10316   Featured
Chemical Structure
497223-25-3
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More than 5000 active chemicals with high quality for research!
Field of application
Cenicriviroc is an orally active, dual CCR2/CCR5 antagonist, and displays potent anti-inflammatory and aninfective activity.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 497223-25-3
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
Synonyms: TAK-652; TAK652; TAK 652; TBR-652; TBR 652; TBR652; Cenicriviroc.
SMILES: O=C(/C1=C/C2=CC(C3=CC=C(OCCOCCCC)C=C3)=CC=C2N(CC(C)C)CCC1)NC4=CC=C([S@](CC5=CN=CN5CCC)=O)C=C4
Formula: C41H52N4O4S
M.Wt: 696.95
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication: [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
Description: Cenicriviroc is an orally active, dual CCR2/CCR5 antagonist, also inhibits both HIV-1 and HIV-2, and displays potent anti-inflammatory and antiinfective activity.
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[1].
In Vitro: Cenicriviroc prevents human immunodeficiency virus type 1 (HIV-1) from cellular entry[2]. 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[3].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
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