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首页 / 抑制剂/激动剂 / 蛋白酶 / DPP4 / Alogliptin Benzoate

苯甲酸阿格列汀 /Alogliptin Benzoate {[allProObj[0].p_purity_real_show]}

货号：A420160 同义名： SYR 322;Alogliptin (benzoate salt)

Alogliptin benzoate is the benzoate salt form of alogliptin which is a selective inhibitor of DPP-4 with IC50 of 6.9 nM that exhibits greater selective than DPP-2, DPP-8 and DPP-9.

Alogliptin Benzoate 化学结构 CAS号：850649-62-6
Alogliptin Benzoate 化学结构
CAS号：850649-62-6
Alogliptin Benzoate 3D分子结构
CAS号：850649-62-6
Alogliptin Benzoate 化学结构 CAS号：850649-62-6
Alogliptin Benzoate 3D分子结构 CAS号：850649-62-6
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Alogliptin Benzoate 纯度/质量文件 产品仅供科研

货号：A420160 标准纯度： {[allProObj[0].p_purity_real_show]}
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Alogliptin Benzoate 生物活性

描述 Alogliptin Benzoate (SYR-322) is a potent, selective, and orally active DPP-4 inhibitor with an IC50 of less than 10 nM, showing over 10,000-fold selectivity against DPP-8 and DPP-9. It is used in research related to type 2 diabetes[1].[2].[3].
体内研究

Alogliptin (0.01-1 mg/kg; orally) results in dose-dependent improvements in glucose tolerance and elevates plasma insulin levels in female Wistar fatty rats[1].

Alogliptin (40 mg/kg/day for two weeks; orally) decreases infarction size and enhances brain vascular integrity in mice with middle cerebral artery occlusion (MCAO)[3].
体外研究

Alogliptin (1 nM; 5-60 minutes) blocks LPS-induced phosphorylation of ERK in U937 cells[2].

Alogliptin (0.5-5 nM; 24 hours) reduces LPS-induced secretion and mRNA expression of MMP-1, mediated by the ERK pathway, in U937 cells[2].

Alogliptin Benzoate 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02798172 Diabetes Mellitus, Type 2 Not Applicable Completed - -
NCT01990300 - Completed - -
NCT03499704 Diabetes Mellitus, Type 2 Phase 4 Not yet recruiting December 31, 2020 -

Alogliptin Benzoate 参考文献

[1]Feng J, et, al. Discovery of alogliptin: a potent, selective, bioavailable, and efficacious inhibitor of dipeptidyl peptidase IV. J Med Chem. 2007 May 17;50(10):2297-300.

[2]Ta NN, et, al. DPP-4 (CD26) inhibitor alogliptin inhibits TLR4-mediated ERK activation and ERK-dependent MMP-1 expression by U937 histiocytes. Atherosclerosis. 2010 Dec;213(2):429-35.

[3]Hao FL, et, al. The neurovascular protective effect of alogliptin in murine MCAO model and brain endothelial cells. Biomed Pharmacother. 2019 Jan;109:181-187.

Alogliptin Benzoate 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.17mL

0.43mL

0.22mL

10.83mL

2.17mL

1.08mL

21.67mL

4.33mL

2.17mL

Alogliptin Benzoate 技术信息

CAS号850649-62-6
分子式C25H27N5O4
分子量 461.513
别名 SYR 322;Alogliptin (benzoate salt)
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,2-8°C
溶解度

DMSO: 25 mg/mL(54.17 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 14 mg/mL(30.34 mM)，配合低频超声，并水浴加热至45℃助溶
动物实验配方

0.5% methylcellulose+water 30 mg/mL suspension

Tags: Alogliptin Benzoate | SYR 322;Alogliptin (benzoate salt) | DPP4 | AmBeed-信号通路专用抑制剂 | Alogliptin Benzoate 纯度/质量文件 | Alogliptin Benzoate 生物活性 | Alogliptin Benzoate 临床数据 | Alogliptin Benzoate 参考文献 | Alogliptin Benzoate 实验方案 | Alogliptin Benzoate 技术信息

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