阿洛利停
货号：
IA3180
品牌：
Jinpan
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产品简介
| EC | EINECS 821-899-3 |
| 描述 | 是高活性DPP4选择性抑制剂。 |
| 别名 | 阿格列汀;SYR-322 |
| 英文名称 | Alogliptin |
| CAS | 850649-61-5 |
| 分子式 | C18H21N5O2 |
| 分子量 | 339.39 |
| 纯度 | ≥98% |
| 单位 | 瓶 |
| 生物活性 | Alogliptin (SYR-322) is a potent, selective inhibitor of the serine protease dipeptidyl peptidase IV (DPP-4) with IC50 values of 2.63 nM and exhibits greater than 10,000 fold selectivity over the closely related serine proteases DPP-8 and DPP-9.[1-4] |
| In Vitro | Alogliptin is a potent (IC50 < 10 nM) inhibitor of DPP-4 and exhibits greater than 10,000 fold selectivity over the closely related serine proteases DPP-8 and DPP-9[1].Compound 10 is not an inhibitor of CYP-450 enzymes and does not block the hERG channel at concentrations up to 30μM[2]. |
| In Vivo | Absolute oral bioavailability of alogliptin in rats, dogs, and monkeys is 45%, 86%, and 72% to 88%, respectively. After a single oral dose of alogliptin, plasma DPP-4 inhibition is observed within 15 min and maximum inhibition is > 90% in rats, dogs, and monkeys; inhibition is sustained for 12 h in rats (43%) and dogs (65%) and 24 h in monkeys (> 80%). From Emax modeling, 50% inhibition of DPP-4 activity is observed at a mean alogliptin plasma concentration (EC50) of 3.4 to 5.6 ng/ml (10.0 to 16.5 nM) in rats, dogs, and monkeys. In Zucker fa/fa rats, a single dose of alogliptin (0.3, 1, 3, and 10 mg/kg) inhibites plasma DPP-4 (91% to 100% at 2 h and 20% to 66% at 24 h), increases plasma GLP-1 (2- to 3-fold increase in AUC0–20 min) and increases early-phase insulin secretion (1.5- to 2.6-fold increase in AUC0-20 min) and reduces blood glucose excursion (31%–67% decrease in AUC0–90 min) after oral glucose challenge. Alogliptin (30 and 100 mg/kg) has no effect on fasting plasma glucose in normoglycemic rats.[3]. |
| SMILES | O=C(C=C(N1C[C@H](N)CCC1)N(C2=O)CC3=C(C#N)C=CC=C3)N2C |
| 靶点 | Dipeptidyl Peptidase（DPP-4） |
| 数据来源文献 | [1] Huan Y, et al.J Pharmacol Toxicol Methods. 2015;71:8-12. [2] Feng J, et al.J Med Chem. 2007,17;50(10):2297-300. [3] Lee B, et al.Eur J Pharmacol. 2008,28;589(1-3):306-14. |
| 规格 | 5mg |
是高活性DPP4选择性抑制剂。