Sitagliptin

Overview

Sitagliptin (MK-0431) is an orally active and highly selective DPP4 inhibitor with an IC 50 value of 19 nM. Sitagliptin blocks the degradation of glucagon-like peptide-1 ( GLP-1 ) and glucose-dependent insulinotropic peptide ( GIP ) by competing inhibition mechanism ( Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4 . Sitagliptin shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin can be used for the study of 1-type and 2-type diabetes.

Application

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Product Information

• Catalog No.: HY-13749
• CAS No.: 486460-32-6
• Molecular Formula: C16H15F6N5O
• Molecular Weight: 407.31
• Purity: 99.94%
• Storage: Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
• Solubility: ≥ 2.5 mg/mL (6.14 mM); Clear solution
• Availability: In-stock

Source

Original product source