DDD85646 是一种有效的布氏锥虫 N-肉豆蔻酰转移酶抑制剂（TbNMT IC50=2 nm；hNMTIC50=4 nm）。
| Cas No. | 1215010-55-1 |
| 别名 | IMP-366 |
| 化学名 | 2,6-dichloro-4-[2-(1-piperazinyl)-4-pyridinyl]-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)-benzenesulfonamide |
| Canonical SMILES | ClC1=CC(C2=CC=NC(N3CCNCC3)=C2)=CC(Cl)=C1S(NC4=C(C)N(C)N=C4C)(=O)=O |
| 分子式 | C21H24Cl2N6O2S |
| 分子量 | 495.4 |
| 溶解度 | 25mg/ml in DMSO & DMF |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | DDD85646 is a moderately bioavailable pyrazole sulphonamide inhibitor of T. brucei N-myristoyltransferase (TbNMT) with an apparent Ki value of 1.44 nM.1 T. brucei is the parasite responsible for human African trypanosomiasis (HAT), also known as African sleeping sickness, and is transmitted through the tsetse fly. DDD85646 administration in mice (12.5 mg/kg for four days) ameliorated T. brucei in an acute mouse model of HAT.[1] It less potently inhibits growth of T. cruzi (EC50 = 6.9 μM).
Reference:
1. Frearson, J.A., Brand, S., McElroy, S.P., et al. N-myristoyltransferase inhibitors as new leads to treat sleeping sickness. Nature 464(7829), 728-732 (2010). |
