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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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| CCR6 antagonist 1
CCR6 antagonist 1 is a CCR6 antagonist that inhibits the CCL20/CCR6 axis. CCR6 antagonist 1 can be used in the research of autoimmune-mediated inflammatory diseases, such as inflammatory bowel diseases (IBDs). |
| IPG7236
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| CKLF1-C19
CKLF1-C19 is the C-terminal peptide of human chemokine-like factor 1 (CKLF1). |
| Met-RANTES (human)
Met-RANTES (human) is a partial antagonist of CCR5. |
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