JY-2

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

JY-2 是一种中等选择性和具有口服活性的叉头转录因子 O1 (FoxO1) 抑制剂，抑制 FoxO1 转录活性的 IC50为 22 μM。JY-2 对 FoxO3a 和 FoxO4 有中度抑制作用。JY-2 具有抗糖尿病活性。

JY-2 is a moderately selective and orally active Forkhead transcription factor forkhead box O1 (FoxO1) inhibitor that inhibits FoxO1 transcriptional activity with an IC50 of 22 μM. JY-2 shows moderate inhibition against FoxO3a and FoxO4. JY-2 shows anti-diabetic activity.

Real Time qPCRCell Line:HepG2 and INS-1 cells Concentration:10, 50 and 100 μM Incubation Time:24 h Result:Reduced palmitic acid (PA)-induced G6Pase and PEPCK mRNA expression. Inhibited PA-induced lipid accumulation. Reduced PA-induced mRNA expression of ER stress markers (ATF3, CHOP and GRP78).Western Blot Analysis Cell Line:HepG2 cells Concentration:10, 50 and 100 μM Incubation Time:4 h; in the presence of PA (500μM)Result:Increased p-FoxO1 levels in the whole cell lysate with a concurrent reduction in nuclear FoxO1 levels.

Animal Model:C57BL/6J mice Dosage:50, 100, 200 mg/kg Administration:Oral, three times for two days (9:00 AM, 7:00 PM, 9:00 AM on the next day)Result:Improved glucose tolerance. Significantly reduced the expression of G6Pase and PEPCK mRNA in the liver. Enhanced mRNA expression of insulin and PDX-1 in the pancreas.Animal Model:db/db mice and C57BL/6J mice, high fat-diet-induced obese diabetic (DIO) model Dosage:50, 100 mg/kg Administration:Oral, once daily for 4 weeks Result:Decreased the levels of fasting blood glucose, improved glucose tolerance. The expression of ColIV, a fibrosis marker, was also lowered.Animal Model:C57BL/6J mice Dosage:20 mg/kg or 50 mg/kg Administration:IV or PO (Pharmacokinetic Analysis) Result:Showed an overall good pharmacokinetic profile.

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Nuclear Receptor/Transcription Factor

Foxo1

FOXO1

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339103-05-8

292.12

C13H7Cl2N3O

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 125 mg/mL (427.91 mM; 超声助溶 (<60°C)

ClC1=CC(Cl)=C(C=C1)C1=NC(=NO1)C1=NC=CC=C1

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(-20℃)

With Ice Pack

≥ 2 years