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Saxagliptin hydrate

Saxagliptin hydrate (Onglyza 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。

CAS号

945667-22-1

分子式

C18H25N3O2·H2O

主要靶点

DPP-4|Proteasome

仅限科研使用

Cat No : CM03792

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Synonyms

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

验证数据展示

  • CAS No.: 945667-22-1

    Saxagliptin hydrate
    CAS#: 945667-22-1

产品信息

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

CAS号 945667-22-1
分子式 C18H25N3O2·H2O
主要靶点 DPP-4|Proteasome
主要通路 泛素化|蛋白酶体
分子量 333.43
纯度 99.80%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 BMS-477118 hydrate|Onglyza hydrate|沙格列汀单水化合物

靶点活性

DPP4:26 nM

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].

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].

溶解度

Ethanol:61 mg/mL (182.9 mM),H2O:1 mg/mL (3 mM),DMSO:61 mg/mL (182.9 mM)

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)

参考文献

1.Neumiller JJ, et al. Am J Health Syst Pharm. 2010, 67(18):1515-25.
2.Solini A, et al. Vascul Pharmacol. 2016, 76:62-71.
3.Henry RR, et al. Diabetes Obes Metab. 2011, 13(9):850-8.
4.Sbaraglini ML, et al. Eur J Pharmacol. 2014, 727:8-14.

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