沙格列汀 T6203

Product Introduction
Bioactivity


英文名: Saxagliptin

描述: Saxagliptin (BMS-477118) 是一种选择性，可逆性，竞争性和口服活性的二肽基肽酶 4 (DPP-4) (Ki= 0.6-1.3 nM) 抑制剂。Saxagliptin 能够用于 2 型糖尿病的研究。

体外活性: Saxagliptin has an inhibition constant Ki of 1.3 nM for DPP4 inhibition, which is 10-fold more potent than either vildagliptin or sitagliptin (another two DPP4 inhibitors) with Ki of 13 and 18 nM. In addition, Saxagliptin demonstrates greater specificity for DPP4 than for either the DPP8 or DPP9 enzymes (400- and 75- fold, respectively). The active metablite of saxagliptin is two-fold less potent than the parent. Both Saxagliptin and its metabolite are highly selective (>4000-fold) for the prevention of DPP4 compared with a range of other proteases (selectivity of sitagliptin and vildagliptin for DPP4 is >2600 and <250-fold, respectively, compared with DPP8 and DPP9). [2] Saxagliptin reduces the degradation of the incretin hormone glucagon-like peptide-1, thereby enhancing its actions, and is associated with improved β-cell function and suppression of glucagon secretion. [3]

体内活性: Maximal responses of Saxagliptin in glucose excursion in Zuckerfa/fa rats are associated with plasma DPP4 inhibition of approximately 60% vs. control, and no additional antihyperglycemic effects are seen at higher percent inhibition. Saxagliptin is highly effective at eliciting marked dose-dependent enhancements in glucose clearance in the dose range 0.13-1.3 mg/kg in ob/ob mice relative to controls. Saxagliptin dose-dependently elevate plasma insulin significantly at 15 min post-oGTT, with concomitant improvement in the glucose clearance curves at 60 min post-oGTT. [4]

存储条件: store at low temperaturePowder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 59 mg/mL (187.1 mM)
H2O : 58 mg/mL (183.9 mM)
Ethanol : 23 mg/mL (72.9 mM)


关键字: Inhibitor | p-AKT | DPP | β-catenin | Dipeptidyl Peptidase | inhibit | Saxagliptin | insulin | DPP-4 | c-myc | proliferation | glucagon | peptide-1 | BMS477118 | diabetes | glucagon-like | BMS 477118

相关产品: Alogliptin | RA375 | Cilastatin | Lactacystin | AC-55541 | Proteasome-IN-1 | Z-LLY-FMK | Retagliptin Phosphate | Baceridin | Z-Leu-Leu-Tyr-COCHO

相关库: FDA-Approved Drug Library | Drug Repurposing Compound Library | Glycometabolism Compound Library | ReFRAME Related Library | FDA-Approved & Pharmacopeia Drug Library | Human Metabolite Library | Inhibitor Library | Highly Selective Inhibitor Library | EMA Approved Drug Library | Orally Active Compound 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