GLUT inhibitor-1

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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 GLUT1GLUT3IC50s 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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