1. Apoptosis Metabolic Enzyme/Protease Immunology/Inflammation TGF-beta/Smad Stem Cell/Wnt
  2. Apoptosis Mitochondrial Metabolism Phosphodiesterase (PDE) COX TGF-beta/Smad
  3. Hydronidone

Hydronidone 是一种有口服活性的吡啶衍生物。Hydronidone 是磷酸二酯酶-4 (PDE4) 和环加氧酶 (COX) 以及 TGF-β 的抑制剂。Hydronidone 可诱发线粒体功能障碍,引发细胞凋亡 (apoptosis)。Hydronidone 可用于肝纤维化、抗炎和抗癌研究。

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Hydronidone Chemical Structure

Hydronidone Chemical Structure

CAS No. : 851518-71-3

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Hydronidone is an orally active pyridine derivative. Hydronidone is an inhibitor of phosphodiesterase-4 (PDE4) and cyclo-oxygenase (COX) as well as TGF-β. Hydronidone induces mitochondrial dysfunction and triggers apoptosis. Hydronidone can be used for liver fibrosis, anti-inflammation and anti-cancer study[1][2][3].

体外研究
(In Vitro)

Hydronidone (200-400 μM) 抑制肝星状细胞 (HSCs) 的活化,并通过调节 Smad7 表达来抑制肝纤维化[1]
Hydronidone (400 μM) 在 HSC 中通过 Smad7 泛素-蛋白酶体依赖性途径促进 TGFβRI 降解[1]
Hydronidone (400 μM, 24 小时) 在 LX-2 细胞中通过线粒体 (内在) 途径显著促进活化肝星状细胞 (aHSC) 的细胞凋亡[2]
Hydronidone (400 μM, 24 小时) 触发内质网应激 (ERS),随后激活 IRE1α-ASK1-JNK 通路[2]

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

Apoptosis Analysis[2]

Cell Line: LX-2 cells
Concentration: 400 μM
Incubation Time: 24 h
Result: Increased the number of apoptotic cells co-treated with TGF-β1.
Reversed the effect of TGF-β1 treatment which induced activation of HSCs as evidenced by increased expression of α-SMA and COL1A1 at both the protein and RNA levels.
Decreased the expression of Bcl-2 and increased the expression of Bax at both the protein and mRNA levels.
Significantly promoted the flow of cytochrome c from the mitochondria to the cytoplasm, indicating impairment of mitochondrial outer membrane permeabilization (MOMP).
Upregulated cleaved-caspase-3/full-length caspase-3 ratio.

Western Blot Analysis[2]

Cell Line: LX-2 cells (hepatic stellate cells)
Concentration: 400 μM
Incubation Time: 24 h
Result: Reversed the effect of TGF-β1-induced activation of HSCs as evidenced by increased expression of α-SMA and COL1A1 at both the protein and RNA levels.
Decreased the expression of Bcl-2 and increased the expression of Bax at both the protein and mRNA levels.
Expression of Bip was significantly upregulated at both the protein and mRNA levels.
Increased the phosphorylated IRE1α (p-IRE1α) level.
Upregulated the level of p-ASK1 and p-JNK, two downstream factors of p-IRE1α.
体内研究
(In Vivo)

Hydronidone (50-100 mg/kg;口服) 可改善 CCl4 和 DDC 诱导的小鼠肝纤维化和肝损伤[1]
Hydronidone 在 CCl4 和 DDC 诱导的小鼠肝纤维化模型中显著促进活化肝星状细胞 (aHSC) 的凋亡[2]

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

Animal Model: Five-week-old male C57BL/6J mice (intraperitoneally injected with 10% carbon tetrachloride (CCl4) in corn oil at 5 μL/g of body weight, three times per week, for 6 weeks; or fed a diet containing 1% 3,5-diethoxycarbonyl-1,4-dihydrocollidine (DDC) for 4 weeks)[1]
Dosage: 50, 100 mg/kg
Administration: Oral gavage (p.o.)
Result: The levels of hepatic inflammatory infiltration were improved.
Significantly reduced the collagen fibre content.
Decreased the hepatic hydroxyproline content.
Significantly reduced the mRNA levels of fibrosis-related genes, including Acta2, Col1a1, Col3a1, Mmp9 and Timp1.
Reduced the levels of α-SMA and collagen 1 (Col1) in liver tissues.
Upregulated Smad7 protein expression.
Clinical Trial
分子量

201.22

Formula

C12H11NO2

CAS 号
性状

固体

颜色

Off-white to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
细胞实验: 

DMSO 中的溶解度 : 100 mg/mL (496.97 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 4.9697 mL 24.8484 mL 49.6968 mL
5 mM 0.9939 mL 4.9697 mL 9.9394 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 (protect from light)。-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

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

纯度: 99.71%

参考文献

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 (protect from light)。-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 4.9697 mL 24.8484 mL 49.6968 mL 124.2421 mL
5 mM 0.9939 mL 4.9697 mL 9.9394 mL 24.8484 mL
10 mM 0.4970 mL 2.4848 mL 4.9697 mL 12.4242 mL
15 mM 0.3313 mL 1.6566 mL 3.3131 mL 8.2828 mL
20 mM 0.2485 mL 1.2424 mL 2.4848 mL 6.2121 mL
25 mM 0.1988 mL 0.9939 mL 1.9879 mL 4.9697 mL
30 mM 0.1657 mL 0.8283 mL 1.6566 mL 4.1414 mL
40 mM 0.1242 mL 0.6212 mL 1.2424 mL 3.1061 mL
50 mM 0.0994 mL 0.4970 mL 0.9939 mL 2.4848 mL
60 mM 0.0828 mL 0.4141 mL 0.8283 mL 2.0707 mL
80 mM 0.0621 mL 0.3106 mL 0.6212 mL 1.5530 mL
100 mM 0.0497 mL 0.2485 mL 0.4970 mL 1.2424 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.

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产品名称:
Hydronidone
目录号:
HY-100438
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