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Vildagliptin (LAF-237)
DPP-4抑制剂,Vildagliptin (LAF-237; NVP-LAF 237)能抑制DPP-4,IC50为2.3 nM。
目录号: PC15656 纯度: ≥98%
CAS No. :274901-16-5
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PC15656-10mg 10mg ¥588.00 请登录
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中文名称
Vildagliptin (LAF-237)
中文别名
维达列汀;(-)-(2S)-1-[[(3-羟基三环[3.3.1.1[3,7]]硅烷-1-基)氨基]乙酰基]吡咯烷-2-甲腈;维他列汀;(-)-(2S)-1-[[(3-羟基三环[3.3.1.1[3,7]]癸烷-1-基)氨基]乙酰基]吡咯烷-2-甲腈;维格列汀;维达利汀;维他列汀S型;维达列汀(维达列汀);维达列汀S型;维达列汀标准品及杂质;维达列汀原药;维达列汀杂质;维达列汀杂质、标准品;维格列汀标准品;维格列汀杂质对照品;他地那兰;维达列汀 维他列汀;(-)-(2S)-1-[[(3-羟基三环[3.3.1.1(3,7)]癸烷-1-基)氨基]乙酰基]吡咯烷-2-甲腈
英文名称
Vildagliptin (LAF-237)
英文别名
Vildagliptin;Vildagliptin (NVP-LAF 237);(-)-(2S)-1-[[(3-Hydroxytricyclo[3.3.1.1[3,7]]dec-1-yl)amino]acetyl]pyrrolidine-2-carbonitrile;2-Pyrrolidinecarbonitrile, 1-(((3-hydroxytricyclo(3.3.1.13,7)dec-1-yl)amino)acetyl)-, (2S)-;Galvus;Laf 237;Unii-I6B4B2U96p;Vildagliptin (LAF-237);2-Pyrrolidinecarbonitrile, 1-[2-[(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)amino]acetyl]-, (2S)-;Vildagliptin (LAF237,Galvus®,Zomelis®);Vildagliptin iMpurity;NVP-LAF 237;2-Pyrrolidinecarbonitrile,1-[[(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)amino]acetyl]-, (2S)- (9CI);(-)-(2S)-1-[[(3-Hydroxytricyclo[3.3.1.1(3,7)]dec-1-yl)amino]acetyl]pyrrolidine-2-carbonitrile;Xiliarx;Jalra;Equa;LAF237;(2S)-1-[2-[(3-hydroxy-1-adamantyl)amino]acetyl]pyrrolidine-2-carbonitrile;I6B4B2U96P;(2S)-1-{2-[(3-hydroxyadamantan-1-yl)amino]acetyl}pyrrolidine-2-carbonitrile;(2S)-1-[N-(3-Hydroxyadamantan-1-yl)glycyl]pyrrolidine-2-carbonitrile;(S)-1-[2-[(3-Hy
Cas No.
274901-16-5
分子式
C17H25N3O2
分子量
303.40
包装储存
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
生物活性

Vildagliptin (LAF237) is a potent, stable, selective dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 3.5 nM in human Caco-2 cells. Vildagliptin possesses excellent oral bioavailability and potent antihyperglycemic activity.

性状

Solid

IC50 & Target[1][2]

IC50: 3.5 nM (DPP-IV, in human Caco-2 cells)

体外研究(In Vitro)

Vildagliptin promotes beta cell survival by inhibiting cell apoptosis. Vildagliptin also promotes cell proliferation.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Vildagliptin (35 mg/kg; once daily by oral gavage) increases plasma active GLP-1 levels in islets of db/db mice.
Vildagliptin (10 μmol/kg; orally) significantly decreases glucose excursions and stimulate insulin secretion in obese male Zucker rats.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male db/db mice (BKS) and wildtype mice
Dosage: 35 mg/kg
Administration: Oral gavage; once daily; for 6 weeks
Result: Increased plasma active GLP-1 levels (22.63±1.19 vs. 11.69±0.44).
Animal Model: Obese male Zucker rats
Dosage: 10 μmol/kg (Pharmacokinetic Analysis)
Administration: Orally
Result: Significantly decreased glucose excursions and stimulate insulin secretion.
运输条件

Room temperature or refrigerated transportation.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
ClinicalTrial
参考文献
溶解度数据
体外研究: 

H2O : 50 mg/mL (164.80 mM; Need ultrasonic)

配制储备溶液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.2960 mL 16.4799 mL 32.9598 mL
5 mM 0.6592 mL 3.2960 mL 6.5920 mL
10 mM 0.3296 mL 1.6480 mL 3.2960 mL
*

产品不同,其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液;配成溶液后,建议分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,建议在 6 个月内使用,-20°C 储存时,建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    建议依照次序添加每种溶剂: PBS

    Solubility: 100 mg/mL (329.60 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

*
搜索质检报告(COA)

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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The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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