|
|
| | TAK-220 Basic information |
| Product Name: | TAK-220 | | Synonyms: | TAK-220;1-ACETYL-N-(3-(4-(4-CARBAMOYLBENZYL)PIPERIDIN-1-YL)PROPYL)-N-(3-CHLORO-4-METHYLPHENYL)PIPERIDINE-4-CARBOXAMIDE;TAK 220;TAK220;4-Piperidinecarboxamide, 1-acetyl-N-[3-[4-[[4-(aminocarbonyl)phenyl]methyl]-1-piperidinyl]propyl]-N-(3-chloro-4-methylphenyl)- | | CAS: | 333994-00-6 | | MF: | C31H41ClN4O3 | | MW: | 553.14 | | EINECS: | | | Product Categories: | | | Mol File: | 333994-00-6.mol |  |
| | TAK-220 Chemical Properties |
| Melting point | 166-167 °C(Solv: ethyl acetate (141-78-6); ethanol (64-17-5)) | | Boiling point | 757.8±60.0 °C(Predicted) | | density | 1.208±0.06 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | DMSO: soluble | | form | A crystalline solid | | pka | 16.16±0.50(Predicted) |
| | TAK-220 Usage And Synthesis |
| Description | TAK-220 is an orally bioavailable antagonist of chemokine (C-C motif) receptor 5 (CCR5). It binds to CCR5 (IC50 = 3.5 nM for the human receptor in CHO cells), but not CCR1, CCR2b, CCR3, CCR4, or CCR7. TAK-220 inhibits the binding of chemokine (C-C motif) ligand 5 (CCL5) and CCL3 to CCR5 (IC50s = 3.5 and 1.4 nM, respectively) but does not inhibit binding of CCL4. It inhibits HIV-1 envelope-mediated membrane fusion in a macrophage (M-tropic) R5, but not in a T cell (T-tropic) X4, strain of HIV-1 (IC50s = 0.42 and >1,000 nM, respectively). TAK-220 inhibits the replication of six strains of R5 HIV-1 clinical isolates (EC90 overall mean = 13 nM) and the R5 JR-FL laboratory-adapted strain (EC50 = 0.6 nM), but not of X4 HIV-1 clinical isolates or the X4 IIIB laboratory-adapted strain (EC50s = >10,000 nM for both), in human peripheral blood mononuclear cells (PBMCs). |
| | TAK-220 Preparation Products And Raw materials |
|