产品说明书

Alogliptin Benzoate

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Chemical Structure| 850649-62-6 同义名 : SYR 322;Alogliptin (benzoate salt)
CAS号 : 850649-62-6
货号 : A420160
分子式 : C25H27N5O4
纯度 : 97%
分子量 : 461.513
MDL号 : MFCD09833195
存储条件:

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月

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

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].
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 -
实验方案
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

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.