CAS |
No.1029877-94-8 |
中文名称 |
琥珀酸曲格列汀 |
英文名称 |
Trelagliptin Succinate |
别名 |
;Trelagliptin(succinate);SYR472succinate;SYR472;Trelagliptinsuccinate[USAN];N-Tosylbenzylamine; |
分子式 |
C22H26FN5O6 |
分子量 |
475.47 |
溶解性 |
Soluble in DMSO ≥5mg/mL |
纯度 |
≥98% |
外观(性状) |
White to off-white Solid |
储存条件 |
Powder:-20℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year |
运输条件 |
冷藏运输 |
MDL |
MFCD22665720 |
SMILES |
CN1C(=O)C=C(N(C1=O)CC2=C(C=CC(=C2)F)C#N)N3CCC[C@H](C3)N.C(CC(=O)O)C(=O)O |
靶点 |
Dipeptidyl Peptidase(DPP-4) |
通路 |
Metabolic Enzyme&Protease |
背景说明 |
是长效的DPP-4抑制剂。 |
生物活性 |
Trelagliptin (SYR-472) succinate is a potent, orally active and highly selective DPP-4 inhibitor with an IC50 of 4 nM. Trelagliptin succinate improves glycemic control in vivo and can be used for the study of type 2 diabetes mellitus (T2DM)[1]. |
IC50 |
IC50: 4nM(DPP-4)[1] |
In Vitro |
Dipeptidyl peptidase-4(DPP-4)is one of the widely explored novel targets for type 2 diabetes mellitus(T2DM)strategy to preserve the endogenous glucagon like peptide(GLP)-1 activity by inhibiting the DPP-4 action[1]. |
In Vivo |
Trelagliptin(oral gavage; 7 mg/kg; single dose)shows sustained PD effect in dogs and gives >80% inhibition of DPP-4 activity even after 24h[1]. |
数据来源文献 |
[1]. Bhumika D Patel, et al. Recent approaches to medicinal chemistry and therapeutic potential of dipeptidyl peptidase-4 (DPP-4) inhibitors. Eur J Med Chem. 2014 Mar 3;74:574-605. |
规格 |
1mg 5mg 10mg 25mg 50mg 100mg |
单位 |
瓶 |