产品
编 号：F757591
分子式：C13H7Cl2N3O
分子量：292.12
分子式：C13H7Cl2N3O
分子量：292.12
产品类型
规格
价格
是否有货
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
50mg
询价
询价
100mg
询价
询价
结构图
CAS No: 339103-05-8
产品详情
生物活性：
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.
体内研究：
JY-2 (50-200 mg/kg; oral; 3 times for two days or daily for 4 weeks) 在小鼠中显示抗糖尿病作用。Pharmacokinetic parameters of JY-2Parametersi.v. (20 mg/kg) p.o. (50 mg/kg)
AUCall (ng·h/mL)5017 ± 103812270 ± 2775
AUCinf.obs (ng·h/mL)5030 ± 103712400 ± 2753
Cmax (ng/mL)10790 ± 32696826 ± 2342
Tmax (h)0.1 ± 0.10.8 ± 0.7
T1/2 (h)0.8 ± 0.21.3 ± 0.4
MRTinf.obs (h)0.7 ± 0.12.0 ± 0.1
F (%)97.8
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.
体外研究：
JY-2 (10-100 μM; 24 h) 降低棕榈酸 (PA;HY-N0830) 诱导的 HepG2 和 INS-1 细胞脂毒性。
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.
体内研究：
JY-2 (50-200 mg/kg; oral; 3 times for two days or daily for 4 weeks) 在小鼠中显示抗糖尿病作用。Pharmacokinetic parameters of JY-2Parametersi.v. (20 mg/kg) p.o. (50 mg/kg)
AUCall (ng·h/mL)5017 ± 103812270 ± 2775
AUCinf.obs (ng·h/mL)5030 ± 103712400 ± 2753
Cmax (ng/mL)10790 ± 32696826 ± 2342
Tmax (h)0.1 ± 0.10.8 ± 0.7
T1/2 (h)0.8 ± 0.21.3 ± 0.4
MRTinf.obs (h)0.7 ± 0.12.0 ± 0.1
F (%)97.8
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.
体外研究：
JY-2 (10-100 μM; 24 h) 降低棕榈酸 (PA;HY-N0830) 诱导的 HepG2 和 INS-1 细胞脂毒性。
产品资料
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