SB742457是5-HT6受体拮抗剂,pKi为9.63,比对其它受体的抑制性高100倍以上。
SB742457 is a highly selective 5-HT6 receptor antagonist with pKi of 9.63, exhibits >100-fold selectivity over other receptors. Phase 2.
1.5 mg/kg 口服处理
动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数 | |
例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。
[1] Chuang ATT, et al. Alzheimers Dement, 2006, 2, S631–S632 (abstract).
分子式 C19H19N3O2S |
分子量 353.44 |
CAS号 607742-69-8 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 200 mM |
Water <1 mg/mL |
Ethanol 5 mM |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT00710684 | Mild-to-moderate Alzheimer's Disease|Alzheimer's Disease | Drug: SB-742457 15mg|Drug: SB-742457 35mg|Drug: Placebo|Drug: donepezil 5-10mg | GlaxoSmithKline | Phase 2 | 2008-07-01 | 2012-03-15 |
NCT00348192 | Alzheimer's Disease | Drug: SB-742457|Drug: donepezil | GlaxoSmithKline | Phase 2 | 2006-05-01 | 2009-05-28 |
NCT00551772 | Alzheimer's Disease | Drug: SB-742457 | GlaxoSmithKline | Phase 1 | 2007-08-01 | 2008-12-23 |
NCT00708552 | Alzheimer's Disease | Drug: SB-742457|Drug: Donepezil|Drug: Placebo | GlaxoSmithKline | Phase 2 | 2008-07-01 | 2017-03-21 |
NCT00224497 | Alzheimer's Disease | Drug: SB-742457 | GlaxoSmithKline | Phase 2 | 2005-09-01 | 2009-12-23 |
注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。
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