Alogliptin Benzoate|850649-62-6|(苯甲酸阿格列汀; SYR 322)-陌孚医药/Medlife

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Alogliptin Benzoate (Synonyms: 苯甲酸阿格列汀; SYR 322)

目录号: PL13900 纯度: ≥99%

CAS No. :850649-62-6

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中文名称	Alogliptin Benzoate
中文别名	苯甲酸阿格列汀;2-[[6-[(3R)-3-氨基-1-哌啶基]-3,4-二氢-3-甲基-2,4-二氧代-1(2H)-嘧啶基]甲基]苯甲腈苯甲酸盐;吡格列酮苯酸酯;阿格列汀苯甲酸盐;阿格列汀;阿格列汀盐;Alogliptin benzoate苯甲酸阿格列汀;阿戈列汀;阿格列汀(阿格列汀苯甲酸盐);阿格列汀-13C-D3;苯甲酸阿格利汀
英文名称	Alogliptin Benzoate
英文别名	Alogliptin benzoate;2-[[6-[(3R)-3-Amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]benzonitrile benzoate;2-[[6-[(3R)-3-aMino-1-piperidinyl]-3,4-dihydro-3-Methyl-2,4-dioxo-1(2H)-pyriMidinyl]Methyl]-Benzonitrile Monobenzoate;SYR 322;Nesina;2-[[6-[(3R)-3-aminopiperidin-1-yl]-3-methyl-2,4-dioxopyrimidin-1-yl]methyl]benzonitrile,benzoic acid;2-[6-[3(R)-Aminopiperidin-1-yl]-3-methyl-2,4-dioxo-1,2,3,4-tetrahydropyrimidin-1-ylmethyl]benzonitrile benzoate;alogliptin;Alogliptin (Benzoate);alogliptin monobenzoate;SYR32;Vipidia (TN);Alogliptin Benzoate
Cas No.	850649-62-6
分子式	C₁₈H₂₁N₅O₂^.C₇H₆O₂
分子量	461.51
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情

Alogliptin Benzoate (SYR-322) 是一种有效的、具有选择性口服活性的 DPP-4 的抑制剂，IC₅₀ 值小于 10 nM，比对 DPP-8 和 DPP-9 的抑制性高 10000 倍以上。Alogliptin Benzoate 可用于研究 2 型糖尿病。

生物活性

Alogliptin Benzoate (SYR-322) is a potent, selective and orally active inhibitor of DPP-4 with an IC 50 of <10 nM, and exhibits greater than 10,000-fold selectivity over DPP-8 and DPP-9. Alogliptin Benzoate can be used for the research of type 2 diabetes.

性状

Solid

IC50 & Target[1][2]

IC50: <10 nM (DPP-4)

体外研究(In Vitro)

Alogliptin (1 nM; 5-60 min) inhibits LPS-induced extracellular signal-regulated kinase (ERK) phosphorylation in U937 cells.
Alogliptin (0.5-5 nM; 24 h) inhibits LPS-stimulated MMP-1 secretion and mRNA expression that is mediated by ERK pathway in U937 cells. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Alogliptin (0.01-1 mg/kg; p.o.) produced dose-dependent improvements in glucose tolerance and increased plasma insulin levels in female Wistar fatty rats.
Alogliptin (40?mg/kg/day for 2 weeks; p.o.) reduces infarction area and improves brain vascular integrity in middle cerebral artery occlusion (MCAO) mice. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

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.

溶解度数据	In Vitro: DMSO : 25 mg/mL (54.17 mM; ultrasonic and warming and heat to 60°C)H₂O : 14.29 mg/mL (30.96 mM; ultrasonic and warming and heat to 60°C)

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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