JY-2|cas:339103-05-8|西域试剂

JY-2,99.75%

产品编号：Bellancom-153347| CAS NO：339103-05-8| 分子式：C₁₃H₇Cl₂N₃O| 分子量：292.12

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货号	价格	库存与货期
Bellancom-153347	￥600.00	杭州北京（现货）
Bellancom-153347	￥1000.00	杭州北京（现货）
Bellancom-153347	￥2000.00	杭州北京（现货）
Bellancom-153347	￥3000.00	杭州北京（现货）
Bellancom-153347	￥4500.00	杭州北京（现货）

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JY-2

产品介绍

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。

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。

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Real Time qPCR

Cell 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.

体内研究
(In Vivo)

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-2

Parameters	i.v. (20 mg/kg)	p.o. (50 mg/kg)
AUC_all (ng·h/mL)	5017 ± 1038	12270 ± 2775
AUC_inf.obs (ng·h/mL)	5030 ± 1037	12400 ± 2753
C_max (ng/mL)	10790 ± 3269	6826 ± 2342
T_max (h)	0.1 ± 0.1	0.8 ± 0.7
T_1/2 (h)	0.8 ± 0.2	1.3 ± 0.4
MRT_inf.obs (h)	0.7 ± 0.1	2.0 ± 0.1
F (%)		97.8

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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-2

Parameters	i.v. (20 mg/kg)	p.o. (50 mg/kg)
AUC_all (ng·h/mL)	5017 ± 1038	12270 ± 2775
AUC_inf.obs (ng·h/mL)	5030 ± 1037	12400 ± 2753
C_max (ng/mL)	10790 ± 3269	6826 ± 2342
T_max (h)	0.1 ± 0.1	0.8 ± 0.7
T_1/2 (h)	0.8 ± 0.2	1.3 ± 0.4
MRT_inf.obs (h)	0.7 ± 0.1	2.0 ± 0.1
F (%)		97.8

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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-2

Parameters	i.v. (20 mg/kg)	p.o. (50 mg/kg)
AUC_all (ng·h/mL)	5017 ± 1038	12270 ± 2775
AUC_inf.obs (ng·h/mL)	5030 ± 1037	12400 ± 2753
C_max (ng/mL)	10790 ± 3269	6826 ± 2342
T_max (h)	0.1 ± 0.1	0.8 ± 0.7
T_1/2 (h)	0.8 ± 0.2	1.3 ± 0.4
MRT_inf.obs (h)	0.7 ± 0.1	2.0 ± 0.1
F (%)		97.8

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 125 mg/mL (427.91 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.4233 mL	17.1163 mL	34.2325 mL
5 mM	0.6847 mL	3.4233 mL	6.8465 mL
10 mM	0.3423 mL	1.7116 mL	3.4233 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式