
Cenicriviroc
CAS No. 497223-25-3
Cenicriviroc( TAK-652 | TBR-652 )
Catalog No. M24457 CAS No. 497223-25-3
Cenicriviroc is an orally active, dual antagonist of CCR2/CCR5. It also inhibits both HIV-1 and HIV-2, and displays potent anti-infective and anti-inflammatory activity.
Purity : >98% (HPLC)






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Biological Information
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Product NameCenicriviroc
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NoteResearch use only, not for human use.
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Brief DescriptionCenicriviroc is an orally active, dual antagonist of CCR2/CCR5. It also inhibits both HIV-1 and HIV-2, and displays potent anti-infective and anti-inflammatory activity.
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DescriptionCenicriviroc is an orally active, dual antagonist of CCR2/CCR5. It also inhibits both HIV-1 and HIV-2, and displays potent anti-infective and anti-inflammatory activity.(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.
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In VitroCenicriviroc 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.
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In VivoCenicriviroc (≥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.
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SynonymsTAK-652 | TBR-652
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PathwayAutophagy
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TargetCCR
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RecptorCCR2| CCR5| HIV-1| HIV-2
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Research Area——
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Indication——
Chemical Information
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CAS Number497223-25-3
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Formula Weight696.94
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Molecular FormulaC42H52N4O4
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Purity>98% (HPLC)
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SolubilityDMSO:120 mg/mL (172.19 mM)
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SMILESCCCCOCCOC1=CC=C(C=C1)C2=CC/3=C(C=C2)N(CCC/C(=C3)/C(=O)NC4=CC=C(C=C4)[S@@](=O)CC5=CN=CN5CCC)CC(C)C
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
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
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