磷酸西他列汀 T23358

Product Introduction
Bioactivity


英文名: Sitagliptin phosphate

描述: Sitagliptin phosphate (MK-0431 phosphate) 是一种二肽基肽酶 4 (DPP4) 抑制剂，在 Caco-2 细胞中，IC50值为 19 nM。

体外活性: In vitro: Sitagliptin was a potent inhibitor for DPP-4 with an IC50 of 18 nM. Sitagliptin inhibited DPP-8 (IC50: 48 μM). Sitagliptin showed no effect on several related peptidases, including DPP-9, DPP-II, and aminopeptidase P [1].

体内活性: In free-fed Han-Wistar rats, the ED50 values ??for the inhibition of plasma DPP-4 activity by sitagliptin phosphate were calculated as 7 hours post-dose at 2.3 mg/kg and 24 hours post-dose at 30 mg/kg [1]. A mouse model of streptozotocin-induced type 1 diabetes showed elevated plasma DPP-4 levels, which was significantly suppressed in mice on a sitagliptin phosphate diet. This is achieved through a positive effect on hyperglycemia regulation, possibly by prolonging islet graft survival. The plasma clearance and volume of distribution of sitagliptin phosphate in rats (40-48 mL/min/kg, 7-9 L/kg) were higher than those in dogs (9 mL/min/kg, 3 L/kg); its The half-life is shorter in rats, 2 hours in dogs and 4 hours in dogs[2].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 25 mg/mL(49.47 mM)


关键字: Sitagliptin Phosphate | MK-0431 | MK 0431 | Sitagliptin phosphate | Dipeptidyl Peptidase | MK 0431 Phosphate | MK0431 | Autophagy | Inhibitor | inhibit | MK0431 Phosphate | Sitagliptin | DPP | MK-0431 Phosphate

相关产品: Alogliptin | Sitagliptin | Saikogenin A | Talabostat mesylate | Trelagliptin | DPP-IV-IN-2 | Linagliptin | Saxagliptin | Saxagliptin hydrate | Anagliptin

相关库: Drug Repurposing Compound Library | Anti-Cancer Drug Library | Clinical Compound Library | Bioactive Compounds Library Max | Anti-Cancer Clinical Compound Library | Inhibitor Library | Anti-Cancer Approved Drug Library | EMA Approved Drug Library | Metabolism Compound Library | Protease Inhibitor Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途