Gemigliptin|911637-19-9|(LC15-0444)-陌孚医药/Medlife

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Gemigliptin (Synonyms: LC15-0444)

目录号: PL11593

CAS No. :911637-19-9

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中文名称	Gemigliptin
中文别名	吉格列汀;吉格列汀酒石酸盐
英文名称	Gemigliptin
英文别名	GeMigliptin;1-[(2S)-2-amino-4-[2,4-bis(trifluoromethyl)-6,8-dihydro-5H-pyrido[3,4-d]pyrimidin-7-yl]-4-oxobutyl]-5,5-difluoropiperidin-2-one;Gemigliptin Hydrochloride;Gemigliptin Tartarate;1-[(2S)-2-Amino-4-[5,8-dihydro-2,4-bis(trifluoromethyl)pyrido[3,4-d]pyrimidin-7(6H)-yl]-4-oxobutyl]-5,5-difluoro-2-piperidinone (ACI);Pyrido[3,4-d]pyrimidine, 7-[(3S)-3-amino-4-(5,5-difluoro-2-oxo-1-piperidinyl)-1-oxobutyl]-5,6,7,8-tetrahydro-2,4-bis(trifluoromethyl)- (9CI);1-[(2S)-2-Amino-4-[2,4-bis(trifluoromethyl)-5,8-dihydropyrido[3,4-d]pyrimidin-7(6H)-yl]-4-oxobutyl]-5,5-difluoropiperidin-2-one;1-[(2S)-2-Amino-4-[2,4-bis(trifluoromethyl)-6,8-dihydro-5H-pyrido[3,4-d]pyrimidin-7-yl]-4-oxobutyl]-5,5-difluoropiperidin-2-one;Gemigliptin;Zemiglo
Cas No.	911637-19-9
分子式	C₁₈H₁₉F₈N₅O₂
分子量	489.36
包装储存	Please store the product under the recommended conditions in the Certificate of Analysis.

产品详情

Gemigliptin (LC15-0444) 是一种高度选择性的，可逆的，竞争性的二肽基肽酶 4 (DPP-4) 抑制剂，对人重组 DPP-4 作用的 IC₅₀ 值为 10.3 nM。Gemigliptin 具有很强的抗糖基化特性。Gemigliptin 可用于晚期糖基化终产物 (AGE) 相关的糖尿病并发症的研究。

生物活性

Gemigliptin (LC15-0444 ) is a highly selective, reversible and competitive dipeptidyl peptidase-4 (DPP-4) inhibitor, with an IC 50 of 10.3 nM for human recombinant DPP-4. Gemigliptin exhibits potent anti-glycation properties. Gemigliptin can be used for the research of advanced glycation end products (AGE)-related diabetic complications.

IC50 & Target[1][2]

IC50: 10.3 nM (human recombinant DPP-4)

体外研究(In Vitro)

Gemigliptin dose-dependently inhibits the formation of AGE-BSA with IC50 of 11.69 mM.
Gemigliptin dose-dependently suppressed the cross-linking of preformed AGE-BSA with rat tail tendon collagen with an IC50 of 1.39 mM.
Gemigliptin is a competitive inhibitor with a Ki of 7.25 nM.
has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Gemigliptin (100 mg/kg; i.g.; daily; for 12 weeks) inhibits AGEs formation and AGE cross-links in vivo.
Gemigliptin dose-dependently inhibits plasma DPP-4 activity in rats, dogs, and monkeys.
has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

ClinicalTrial

参考文献

[1]. Jung E, et al. Gemigliptin, a novel dipeptidyl peptidase-4 inhibitor, exhibits potent anti-glycation properties in vitro and in vivo. Eur J Pharmacol. 2014 Dec 5;744:98-102.
[2]. Kim SH, et al. Pharmacological profiles of gemigliptin (LC15-0444), a novel dipeptidyl peptidase-4 inhibitor, in vitro and in vivo. Eur J Pharmacol. 2016 Oct 5;788:54-64.

溶解度数据	In Vitro: DMSO : 50 mg/mL (102.17 mM; Need ultrasonic)配制储备液

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产品使用指南

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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