GLUT inhibitor-1

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

GLUT inhibitor-1 

GLUT inhibitor-1 是一种有效且具有口服活性的葡萄糖转运蛋白抑制剂，靶向 GLUT1 和 GLUT3，IC50s 值分别为 242 nM 和 179 nM。GLUT inhibitor-1 具有研究癌症和自身免疫性疾病的潜力。

GLUT inhibitor-1

GLUT inhibitor-1 Chemical Structure

CAS No. : 2421141-40-2

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生物活性

GLUT inhibitor-1 is a potent and orally active inhibitor of glucose transporters, targeting both GLUT1 and GLUT3, with IC50s of 242 nM and 179 nM, respectively. GLUT inhibitor-1 has the potential for the reaesrch of cancers and autoimmune diseases[1].

IC50 & Target

GLUT1

242 nM (IC50)

GLUT3

179 nM (IC50)

体内研究
(In Vivo)

Summary of the pharmacokinetic parameters of GLUT inhibitor-1 (compound 15b; 30 mg/kg) in mouse and rat[1].

Parameter Mouse Rat
oral Cmax (ng/mL) 2525 1675
oral AUC (ng/mL) 5890 6813
CL (mL/min/kg) 40 37
Vdss (L/Kg) 1.70 4.51
t1/2 (h) 0.785 2.59
F (%) 45.4 49.4
B/Pb 0.05

b: Solubility is determined in PBS buffer solutions.

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

549.67

Formula

C32H35N7O2
CAS 号

2421141-40-2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Liu KG, et al. Discovery and Optimization of Glucose Uptake Inhibitors. J Med Chem. 2020;63(10):5201-5211.

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