Cenicriviroc

SKU: orb1296069

Description

Cenicriviroc (TAK-652) is an orally bioavailable dual CCR2 and CCR5 antagonist. It exhibits anti-HIV-1/2 activity and has been investigated in research for its anti-inflammatory effects in models of liver and kidney fibrosis, both in vitro and in vivo.

Research Area

Immunology & Inflammation, Infectious Disease & Virology, Pharmacology & Drug Discovery, Protein Biochemistry

Key Properties

• CAS Number: 497223-25-3
• MW: 696.94
• Purity: 98.98%
• Formula: C₄₁H₅₂N₄O₄S
• SMILES: CCCCOCCOc1ccc(cc1)-c1ccc2N(CC(C)C)CCC\C(=C/c2c1)C(=O)Nc1ccc(cc1)S(=O)Cc1cncn1CCC
• Target: HIV Protease,CCR
• Solubility: DMSO:120 mg/mL (172.18 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (5.74 mM)

Bioactivity

• Target IC50:
  R5 HIV-1:0.024-0.08 nM (in PBMCs)|R5 HIV-2:0.03-0.98 nM (in PBMCs)|CCR2:5.9 nM|CCR5:0.29 nM
• In Vivo:
  Cenicriviroc (≥20 mg/kg/day) significantly reduces monocyte/macrophage recruitment in vivo and lowers the non-alcoholic fatty liver disease activity score in the NASH model, without affecting body, liver, or kidney weight .
• In Vitro:
  Cenicriviroc prevents 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 .
• Animal Research:
  Male C57BL/6 mice (n=44; 8-10 weeks of age) are allocated to receive treatments via oral gavage (PO) on Days 1-5 in the following groups: non-disease control, vehicle control twice daily (BID), Cenicriviroc 5 mg/kg/day (Cenicriviroc5) BID, Cenicriviroc 20 mg/kg/day (Cenicriviroc20) BID, Cenicriviroc 100 mg/kg/day (Cenicriviroc100) BID, Cenicriviroc20 QD, and positive control (corticosteroid known to reduce inflammation in a variety of animal models) 1 mg/kg QD. On Day 4, peritonitis is induced via IP injection of TG 3.85% (1 mL/animal) 2 hours post-dose in all groups except non-disease controls .

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, HIV, HIV Protease, HIVProtease, HIV-2, HIV-1, Inhibitor, Human immunodeficiency virus, CCR2, CCR, Cenicriviroc, CCR5, CC chemokine receptor, TAK 652, TAK652, TAK-652, TBR 652, TBR652, TBR-652

Compound Identifiers

PubChem CID

5275741