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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Dipeptidyl Peptidase (DPP)-Vildagliptin
Vildagliptin

Chemical Structure : Vildagliptin

CAS No.: 274901-16-5

Vildagliptin (NVP-LAF237, LAF237)

货号: PC-22850Not For Human Use, Lab Use Only.

Vildagliptin (NVP-LAF237, LAF237) is a potent, selective and orally bio-available DPP-4 (DPP-IV) inhibitor with IC50 of 3.5 nM in primary DPP-IV assay in human Caco-2 cells.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Vildagliptin (NVP-LAF237, LAF237) is a potent, selective and orally bio-available DPP-4 (DPP-IV) inhibitor with IC50 of 3.5 nM in primary DPP-IV assay in human Caco-2 cells.
Vildagliptin (NVP-LAF237, LAF237) is a slow-binding DPP IV inhibitor with an association rate constant of 1.4x10(5)M(-1)s(-1) and a K(i) of 17nM.
Vildagliptin (NVP-LAF237, LAF237) is a micromolar inhibitor for dipeptidyl-peptidase 8 and does not significantly inhibit dipeptidyl-peptidase II (EC 3.4.11.2), prolyl oligopeptidase (EC 3.4.21.26), aminopeptidase P (EC 3.4.11.9) or aminopeptidase M (EC 3.4.11.2).
Vildagliptin (NVP-LAF237, LAF237) improves insulin secretion and glucose homeostasis with a profile wholly consistent with increased action of glucagon-like peptide-1.

物理化学性质&存储条件

分子量 303.41
分子式 C17H25N3O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(2S)-{[(3-hydroxyadamantan-1-yl)amino]acetyl}-pyrrolidine-2-carbonitrile

参考文献

1. Villhauer EB, et al. J Med Chem. 2003 Jun 19;46(13):2774-89.

2. Mari A, et al. J Clin Endocrinol Metab. 2005 Aug;90(8):4888-94.

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