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Cenicriviroc (TAK-652) is an orally active, dual CCR2/CCR5 antagonist that inhibits both HIV-1 and HIV-2, exhibiting potent anti-infective and anti-inflammatory activity.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | 59 € | In Stock | |
2 mg | 85 € | In Stock | |
5 mg | 122 € | In Stock | |
10 mg | 194 € | In Stock | |
25 mg | 391 € | In Stock | |
50 mg | 505 € | In Stock | |
100 mg | 729 € | In Stock | |
200 mg | 1.026 € | In Stock | |
1 mL x 10 mM (in DMSO) | 209 € | In Stock |
Description | Cenicriviroc (TAK-652) is an orally active, dual CCR2/CCR5 antagonist that inhibits both HIV-1 and HIV-2, exhibiting potent anti-infective and anti-inflammatory activity. |
Targets&IC50 | CCR5:0.29 nM, CCR2:5.9 nM, R5 HIV-1:0.024-0.08 nM (in PBMCs), R5 HIV-2:0.03-0.98 nM (in PBMCs) |
In vitro | Cenicriviroc prevents 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]. |
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 [1]. |
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 [1]. |
Alias | TBR-652, TAK-652 |
Molecular Weight | 696.94 |
Formula | C41H52N4O4S |
Cas No. | 497223-25-3 |
Smiles | CCCCOCCOc1ccc(cc1)-c1ccc2N(CC(C)C)CCC\C(=C/c2c1)C(=O)Nc1ccc(cc1)S(=O)Cc1cncn1CCC |
Relative Density. | 1.17 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 120 mg/mL (172.19 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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