产品信息
抗原名称
Dipeptidyl Peptidase
商品描述
Anagliptin is a pharmaceutical drug for the treatment of type 2 diabetes mellitus.
分子量
383.45
纯度
>98%
可溶性
DMSO: ≥ 36 mg/mL
In vitro(体外研究)
Anagliptin is a highly selective, potent inhibitor of DPP-IV, with an IC50 of 3.8 nM, and less selective at DPP-8/9 (68, 60 nM, respectively). Anagliptin does not affect CYP3A4, CYP2C19, CYP2C9, CYP1A2, and CYP2D6 (IC50 >10 μM) or CYP3A4, CYP2C8, CYP2C9, and CYP1A2 at 50 μM. Anagliptin hydrochloride does not bind to the hERG channel (E-4031, >90% inhibition at 0.1 μM, IC50 >500 μM in patch clamp using HEK 293 cells). Anagliptin (1-100 μM) dose-dependently suppresses-DPP-4-induced smooth muscle cells (SMCs) proliferation, and reduces TNF-α production in cultured monocytes.
In vivo(体内研究)
Anagliptin (0.3%) alters the quantity and quality of atherosclerotic lesions in apoE-deficient mice, and reduces DPP-4 activity in the plasma, and total cholesterol level, especially VLDL and LDL-C in mice. Anagliptin also decreases α-SMA-positive area and TNF-α-positive lesions in plaque area of apoE-deficient mice. In addition, Anagliptin does not increase the number of circulating endothelial progenitor cells (EPCs) in apoE-deficient mice. Anagliptin (0.3%) decreases the low-density lipoprotein cholesterol and very low-density lipoprotein cholesterol, and also reduces the sterol regulatory element-binding protein-2 messenger ribonucleic acid expression level in mice.
背景
别名
SK-0403
分子式
C19H25N7O2
CAS号
739366-20-2
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
参考图片
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