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)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
2MG 81 In Stock
5MG 116 In Stock
10MG 185 In Stock
25MG 371 In Stock
50MG 479 In Stock
100MG 691 In Stock
200MG Get Quote In Stock
500MG Get Quote In Stock
1G Get Quote In Stock

Biological Information

  • Product Name
    Cenicriviroc
  • Note
    Research use only, not for human use.
  • Brief Description
    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.
  • Description
    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.(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.
  • 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.
  • Synonyms
    TAK-652 | TBR-652
  • Pathway
    Autophagy
  • Target
    CCR
  • Recptor
    CCR2| CCR5| HIV-1| HIV-2
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    497223-25-3
  • Formula Weight
    696.94
  • Molecular Formula
    C42H52N4O4
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO:120 mg/mL (172.19 mM)
  • SMILES
    CCCCOCCOC1=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
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • 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
molnova catalog
related products
  • CCR2 antagonist 3

    CCR2 antagonist 3 is an antagonist of CCR2.

  • CCR2 antagonist 4

    CCR2 antagonist 4 is a potent and specific antagonist of CCR2(IC50s of 180 nM), and potently inhibits MCP-1-induced chemotaxis(IC50 of 24 nM).

  • CCR4 antagonist 3-1

    CCR4 antagonist 3-1 is a less active chemokine receptor 4 (CCR4) antagonist that inhibits [125I]TARC (thymus and activation-regulated chemokine) with an IC50 value of 1.7 μM.