GSK1292263是PR119受体激动剂,可用于2型糖尿病。
GSK1292263 is a novel GPR119 agonist, showing potential for the treatment of type 2 diabetes. Phase 2.
3-30 mg/kg
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] Zhu X, et al. Eur J Med Chem, 2011, 46(7), 2901-2907.
[2] Derek J. Nunez,et al. PLoS One. 2014; 9(4): e92494. Published online 2014 Apr 3. doi: 10.1371/journal.pone.0092494.
分子式 C23H28N4O4S |
分子量 456.56 |
CAS号 1032823-75-8 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 32 mg/mL |
Water <1 mg/mL |
Ethanol <1 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT01101568 | Diabetes Mellitus, Type 2 | Drug: Simvastatin|Drug: Rosuvastatin|Drug: GSK1292263 | GlaxoSmithKline | Phase 1 | 2010-04-01 | 2016-11-30 |
NCT01119846 | Diabetes Mellitus, Type 2 | Drug: GSK1292263|Drug: GSK1292263 matching placebo|Drug: Sitagliptin | GlaxoSmithKline | Phase 2 | 2009-06-01 | 2016-12-01 |
NCT01128621 | Diabetes Mellitus, Type 2 | Drug: GSK1292263|Drug: GSK1292263 matching placebo|Drug: Sitagliptin | GlaxoSmithKline | Phase 2 | 2009-11-01 | 2016-11-30 |
NCT01218204 | Dyslipidaemias | Drug: 10mg atorvastatin|Drug: 80mg atorvastatin|Drug: GSK1292263 Placebo|Drug: 100mg GSK1292263|Drug: 300mg GSK1292263|Drug: 800mg GSK1292263|Drug: 10mg ezetimibe|Other: Washout | GlaxoSmithKline | Phase 2 | 2010-09-01 | 2015-04-27 |
NCT00783549 | Dyslipidaemias | Drug: an undetermined dose of GSK1292263|Drug: ascending dose of GSK1292263|Drug: ascending dose of GSK1292263|Drug: ascending dose of GSK1292263|Drug: ascending dose of GSK1292263 | GlaxoSmithKline | Phase 1 | 2008-09-01 | 2016-10-26 |
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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