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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。

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JY-2 Chemical Structure

JY-2 Chemical Structure

CAS No. : 339103-05-8

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10 mg ￥1000
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25 mg ￥2000
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50 mg ￥3000
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100 mg ￥4500
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Customer Review

JY-2 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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[1].

IC50 & Target

22 μM (FoxO1 transcriptional activity)[1]
体外研究
(In Vitro)

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[1]。

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

JY-2 相关抗体:

Real Time qPCR[1]

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[1]

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[1]。
Pharmacokinetic parameters of JY-2[1]

Parameters i.v. (20 mg/kg) p.o. (50 mg/kg)
AUCall (ng·h/mL) 5017 ± 1038 12270 ± 2775
AUCinf.obs (ng·h/mL) 5030 ± 1037 12400 ± 2753
Cmax (ng/mL) 10790 ± 3269 6826 ± 2342
Tmax (h) 0.1 ± 0.1 0.8 ± 0.7
T1/2 (h) 0.8 ± 0.2 1.3 ± 0.4
MRTinf.obs (h) 0.7 ± 0.1 2.0 ± 0.1
F (%) 97.8

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

Animal Model: C57BL/6J mice[1]
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[1]
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[1]
Dosage: 20 mg/kg or 50 mg/kg
Administration: IV or PO (Pharmacokinetic Analysis)
Result: Showed an overall good pharmacokinetic profile.
分子量

292.12

Formula

C13H7Cl2N3O
CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 100 mg/mL (342.33 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

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
查看完整储备液配制表

* 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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

JY-2 相关分类

完整储备液配制表

* 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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.4233 mL 17.1163 mL 34.2325 mL 85.5813 mL
5 mM 0.6847 mL 3.4233 mL 6.8465 mL 17.1163 mL
10 mM 0.3423 mL 1.7116 mL 3.4233 mL 8.5581 mL
15 mM 0.2282 mL 1.1411 mL 2.2822 mL 5.7054 mL
20 mM 0.1712 mL 0.8558 mL 1.7116 mL 4.2791 mL
25 mM 0.1369 mL 0.6847 mL 1.3693 mL 3.4233 mL
30 mM 0.1141 mL 0.5705 mL 1.1411 mL 2.8527 mL
40 mM 0.0856 mL 0.4279 mL 0.8558 mL 2.1395 mL
50 mM 0.0685 mL 0.3423 mL 0.6847 mL 1.7116 mL
60 mM 0.0571 mL 0.2853 mL 0.5705 mL 1.4264 mL
80 mM 0.0428 mL 0.2140 mL 0.4279 mL 1.0698 mL
100 mM 0.0342 mL 0.1712 mL 0.3423 mL 0.8558 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

JY-2339103-05-8JY2JY 2OtherslipotoxicityHepG2INS-1ColIVG6PasePEPCKATF3CHOPGRP78Inhibitorinhibitorinhibit

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目录号：
HY-153347
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