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Saxagliptin hydrate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Saxagliptin hydrate图片
CAS NO:945667-22-1
包装与价格:
包装价格(元)
5 mg电议
10 mg电议
50 mg电议
100 mg电议
200 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
Onglyza hydrate
沙格列汀单水化合物
BMS-477118 hydrate
产品介绍
Saxagliptin hydrate 是一种选择性,竞争性,可逆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 hydrate 能够用于 2 型糖尿病的研究。

产品描述

Saxagliptin is a selective and reversible DPP4 inhibitor (IC50: 26 nM; Ki: 1.3 nM).

体外活性

In vitro, saxagliptin inhibits FBS-, insulin- and IGF1-induced ERK phosphorylation and cell proliferation, in both MSC and MC3T3E1 preosteoblasts. In the absence of growth factors, saxagliptin has no effect on ERK activation or cell proliferation. In both MSC and MC3T3E1 cells, saxagliptin in the presence of FBS inhibits Runx2 and osteocalcin expression, type-1 collagen production and mineralization, while increasing PPAR-gamma expression[4].

体内活性

Saxagliptin exerts direct beneficial effects on the arterial wall in an animal model of type 2 diabetes by increasing NO availability and improving antioxidant status. Saxagliptin reverses vascular hypertrophic remodeling and ameliorates NO availability in small arteries from db/db mice through the abrogation of NAD(P)H oxidase-driven eNOS uncoupling and by reducing the action of cyclooxygenase-1-derived vasoconstrictors downregulating the expression of thromboxane-prostanoid receptors[2]. DPP-4 inhibition with saxagliptin also improves pancreatic β-cell function in postprandial and fasting states, and decreases postprandial glucagon concentration[3].

细胞实验

Sub-confluent cells are serum-starved overnight and then incubated with 1.5 or 15 μM saxagliptin and/or FBS (1%), insulin (5 ng/mL) or IGF1 (10-8 M) for 24 h (effects on cell proliferation) or 1 h (effects on signal transduction mechanisms). (Only for Reference)

Cas No.

945667-22-1

分子式

C18H27N3O3

分子量

333.432

别名

Onglyza hydrate;沙格列汀单水化合物;BMS-477118 hydrate

储存和溶解度

DMSO:61 mg/mL (182.9 mM)
H2O:1 mg/mL (3 mM)
Ethanol:61 mg/mL (182.9 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years