| CAS NO: | 1029877-94-8 |
| 包装: | 10mg |
| 包装 | 价格(元) |
| 10mg | 电议 |
Trelagliptin succinate（曲格列汀琥珀酸盐）是DPP-4抑制剂，被用作新型长效药物，用于II型糖尿病的治疗。
Trelagliptin(SYR-472) succinate exhibits approximately 4- and 12-fold more potent inhibition against human dipeptidyl peptidase-4 than alogliptin and sitagliptin, respectively, and >10,000-fold selectivity over related proteases including dipeptidyl peptidase-8 and dipeptidyl peptidase-9. Kinetic analysis reveals reversible, competitive and slow-binding inhibition of dipeptidyl peptidase-4 by trelagliptin (t1/2 for dissociation ≈ 30 minutes). X-ray diffraction data indicates a non-covalent interaction between dipeptidyl peptidase and trelagliptin.
Currently, all available DPP-4 inhibitors are dosed once-daily. Phase III clinical studies with trelagliptin in Japan to evaluate its safety and efficacy in a once-weekly oral treatment regimen.
| 分子量 | 475.47 |
| 分子式 | C18H20FN5O2.C4H6O4 |
| CAS号 | 1029877-94-8 |
| 纯度 | >98% |
| 溶解性（25°C） | DMSO 90 mg/mL Water 90 mg/mL |
| 储存和运输条件 | 固体粉末： -20°C 冷藏长期储存 常温运输及临时存放 |
| 小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 | |
| 重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| 体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km系数 | 3 | 6 | 12 | 8 | 5 | 20 |
| 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，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。
以下数据基于产品分子量，对于特殊产品，请参照COA中的储备液配制条件和说明进行操作。
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.1032 mL | 10.5159 mL | 21.0318 mL |
| 5 mM | 0.4206 mL | 2.1032 mL | 4.2064 mL |
| 10 mM | 0.2103 mL | 1.0516 mL | 2.1032 mL |
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