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TAK-779 is a potent and selective nonpeptide antagonist of CCR5, with a Ki of 1.1 nM for CCR5. TAK-779 strongly inhibited migration of CXCR3/CCR5 bearing CD4+, CD8+ and CD11b+ leukocytes to the CNS. TAK-779 effectively and selectively inhibits R5 HIV-1, with EC50 and EC90 of 1.2 nM and 5.7 nM, respectively, in MAGI-CCR5 cells.
In vivo, TAK-779 (10 mg/kg per day, s.c.) significantly prolongs the allograft survival of the rat intestinal transplantation model. TAK-779 (150 µg per mouse, s.c.) supppresses the development of experimental autoimmune encephalomyelitis (EAE) in myelin oligodendrocyte glycoprotein (MOG)-immunized C57BL/6 mice. Treatment with TAK-779 reduced incidence and severity of experimental autoimmune encephalomyelitis.
| Molecular Weight | 531.13 |
| Formula | C33H39ClN2O2 |
| CAS Number | 229005-80-5 |
| Solubility (25°C) | DMSO: ≥ 20 mg/mL Water: ≥ 10 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related CCR Products |
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| Maraviroc
Maraviroc (UK-427857) is a selective CCR5 antagonist with potent anti-human immunodeficiency virus type 1 (HIV-1) activity and favorable pharmacological properties. |
| Vicriviroc Malate
Vicriviroc (SCH 417690) is a pyrimidine CCR5 entry inhibitor of HIV-1 with IC50 of 0.91 nM. |
| Bindarit
Bindarit (AF2838) is a selective inhibitor of the monocyte chemotactic proteins MCP-1/CCL2, MCP-3/CCL7 and MCP-2/CCL8. Bindarit also has anti-inflammatory activity. |
| BMS-813160
BMS-813160 is the first dual CCR2/CCR5 antagonist. BMS-813160 binds with CCR2, CCR5, CCR1, CCR4 and CXCR2 with IC50s of 6.2 nM, 3.6 nM, ＞25 μM, ＞40 μM and ＞40 μM, respectively. |
| INCB3284 dimesylate
INCB 3284 dimesylate is a potent, selective and orally bioavailable hCCR2 antagonist with IC50 of 3.7 nM. |
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