Bioactivity | Cadisegliatin (TTP-399) is a potential, orally active liver-selective glucokinase (GK) activator. Cadisegliatin has antihyperglycaemic activity. Cadisegliatin can be used for the research of type 2 diabetes[1][2]. |
Invitro | Cadisegliatin (TTP-399) 增加大鼠肝细胞的葡萄糖代谢,15 nM 葡萄糖中乳酸和糖原的 EC50 值分别为 2.39 μM 和 2.64 μM [2]. |
In Vivo | TTP399(200 mg/kg,口服,口服)对禁食大鼠的血浆葡萄糖和胰岛素没有影响[2]。TTP399(75 或 150 mg/kg,每天,持续 4 周)改善 ob/ob 小鼠模型的葡萄糖稳态[2]。TTP399(50 mg/kg,每天,持续 13 周)在小型猪模型的口服葡萄糖耐量试验 (OGTT) 期间有效降低血浆葡萄糖[2] 。 Animal Model: |
Name | Cadisegliatin |
CAS | 859525-02-3 |
Formula | C21H33N3O4S2 |
Molar Mass | 455.63 |
Appearance | Solid |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
Reference | [1]. International Nonproprietary Names for Pharmaceutical Substances (INN) [2]. Adrian Vella, et al. Targeting hepatic glucokinase to treat diabetes with TTP399, a hepatoselective glucokinase activator. Sci Transl Med. 2019 Jan 16;11(475):eaau3441. |