Vildagliptin (Synonyms:维格列汀; LAF237; NVP-LAF 237)
目录号 : KM10868 CAS No. : 274901-16-5 纯度 : 98%

Vildagliptin (LAF237) 是一种有效且稳定的选择性二肽基肽酶IV (DPP-IV) 抑制剂,在人 Caco-2 细胞中抑制 DPP-IV 的 IC50 为 3.5 nM。Vildagliptin 具有出色的口服生物利用度和有效的降血糖活性。

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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.

体外研究

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

体内研究

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.

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.
分子式
C17H25N3O2
分子量
303.40
CAS号
274901-16-5
中文名称
维达列汀;维格列汀
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

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

配制储备液
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
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,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,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:
  • 1.

    Vildagliptin is added to drinking water at a concentration of 150 mg/L for rats or 300 mg/L for mice.

临床试验
科研文献
The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
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