生物活性
Sitagliptin phosphate monohydrate是二肽基肽酶-4（DPP-4）类的抗糖尿病（抗高血糖）药物。 DPP-4酶的抑制作用被认为会增加胰高血糖素样肽1（GLP-1），从而抑制胰高血糖素释放，刺激胰岛素释放并降低血糖。
靶点信息
| DPP-4 (Cell-free assay) | | | | |
| 19 nM | | | | |
化学数据
| 目录号 | A10848 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 523.3 |
| Formula | C16H15F6N5O.H3PO4.H2O |
| Purity | >99% |
| Storage | Store lyophilized at -20ºC, keep desiccated.
In lyophilized form, the chemical is stable for36 months.
In solution, store at -20ºC and use within3 monthsto prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles. |
| CAS No. | 654671-77-9 |
| Synonyms | Januvia, MK-0431 |
| SMILES | C1CN2C(=NN=C2C(F)(F)F)CN1C(=O)C[C@@H](CC3=CC(=C(C=C3F)F)F)N.O.OP(=O)(O)O |
溶解度
| In vitro (25°C) | DMSO | 85 mg/mL (162.42 mM) |
| Water | 35 mg/mL (66.88 mM) |
| Ethanol | Insoluble |
| In vivo | Saline | 28 mg/mL |
*<1 mg/ml means slightly soluble or insoluble.
*Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
储备液配制
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
| 0.1 mM | 19.11 mL | 95.55 mL | 191.09 mL |
| 0.5 mM | 3.82 mL | 19.11 mL | 38.22 mL |
| 1 mM | 1.91 mL | 9.55 mL | 19.11 mL |
| 5 mM | 0.38 mL | 1.91 mL | 3.82 mL |
*The above data is based on the productmolecular weight 523.3 . Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
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