1. Metabolic Enzyme/Protease NF-κB Membrane Transporter/Ion Channel Neuronal Signaling Immunology/Inflammation
  2. Glutathione S-transferase NF-κB Calcium Channel NO Synthase
  3. Ethacrynic acid

Ethacrynic acid  (Synonyms: 依他尼酸; Etacrynic acid)

目录号: HY-B1640 纯度: 99.90%
COA 产品使用指南

Ethacrynic acid 具有抗炎抗癌活性。Ethacrynic acid 是一种口服有效的利尿剂。Ethacrynic acid 是谷胱甘肽 S-转移酶 (GSTs)Wnt 信号通路的抑制剂。Ethacrynic acid 是一种放射增敏剂。Ethacrynic acid 可以抑制小鼠气道平滑肌 (ASM) 收缩。 Ethacrynic acid 可以增加眼睛房水流出用于青光眼的研究。

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Ethacrynic acid Chemical Structure

Ethacrynic acid Chemical Structure

CAS No. : 58-54-8

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥610
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50 mg ¥550
In-stock
100 mg ¥950
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200 mg   询价  
500 mg   询价  

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Customer Review

Other Forms of Ethacrynic acid:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Ethacrynic acid has anti-inflammatory and anticancer activity. Ethacrynic acid is an orally active diuretic. Ethacrynic acid is an inhibitor of glutathione S-transferase (GSTs) and Wnt signaling pathways. Ethacrynic acid is a radiosensitizer. Ethacrynic acid can inhibit airway smooth muscle (ASM) contraction in mice. Ethacrynic acid can increase the outflow of aqueous humor from the eye for the study of glaucoma[1][2][3][4][5][6][7][8][9].

IC50 & Target

L-type calcium channel

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO-K1 EC50
56 μM
Compound: 1
Cytotoxicity against CHO-K1 cells by Alamar blue assay
Cytotoxicity against CHO-K1 cells by Alamar blue assay
[PMID: 16962325]
HCT-116 IC50
30.22 μM
Compound: EA
Cytotoxic activity against human HCT116 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
Cytotoxic activity against human HCT116 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
[PMID: 27156773]
HCT-116 IC50
75 μM
Compound: 1; EA
Antiproliferative activity against human HCT116 cells after 24 to 72 hrs by MTS assay
Antiproliferative activity against human HCT116 cells after 24 to 72 hrs by MTS assay
[PMID: 27448922]
HL-60 IC50
38 μM
Compound: 1; EA
Cytotoxicity against human HL60 cells assessed as reduction in cell viability after 24 hrs by MTS assay
Cytotoxicity against human HL60 cells assessed as reduction in cell viability after 24 hrs by MTS assay
[PMID: 27448922]
HL-60 GI50
44.2 μM
Compound: EA
Growth inhibition of human HL60 cells after 72 hrs by trypan blue staining
Growth inhibition of human HL60 cells after 72 hrs by trypan blue staining
[PMID: 22370342]
HL-60 GI50
44.2 μM
Compound: EA
Antiproliferative activity against human HL60 cells after 72 hrs
Antiproliferative activity against human HL60 cells after 72 hrs
[PMID: 17287120]
HL-60 GI50
45 μM
Compound: EA
Growth inhibition of human HL60 cells by hemocytometry
Growth inhibition of human HL60 cells by hemocytometry
[PMID: 20055416]
HL-60 IC50
46 μM
Compound: 1; EA
Antiproliferative activity against human HL60 cells after 24 to 72 hrs by MTS assay
Antiproliferative activity against human HL60 cells after 24 to 72 hrs by MTS assay
[PMID: 27448922]
HT-1080 IC50
54.53 μM
Compound: EA
Cytotoxic activity against human HT1080 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
Cytotoxic activity against human HT1080 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
[PMID: 27156773]
HT-29 IC50
62.39 μM
Compound: EA
Cytotoxic activity against human HT-29 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
Cytotoxic activity against human HT-29 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
[PMID: 27156773]
KB IC50
11 μM
Compound: 1; EA
Antiproliferative activity against human KB cells after 24 to 72 hrs by MTS assay
Antiproliferative activity against human KB cells after 24 to 72 hrs by MTS assay
[PMID: 27448922]
MCF7 IC50
28.92 μM
Compound: EA
Cytotoxic activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
Cytotoxic activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
[PMID: 27156773]
MCF7 IC50
41 μM
Compound: 1; EA
Antiproliferative activity against human MCF7 cells after 24 to 72 hrs by MTS assay
Antiproliferative activity against human MCF7 cells after 24 to 72 hrs by MTS assay
[PMID: 27448922]
MDA-MB-231 IC50
45.24 μM
Compound: EA
Cytotoxic activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
Cytotoxic activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
[PMID: 27156773]
MDA-MB-468 IC50
81.45 μM
Compound: EA
Cytotoxic activity against human MDA-MB-468 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
Cytotoxic activity against human MDA-MB-468 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
[PMID: 27156773]
NCI-H1299 IC50
44.29 μM
Compound: EA
Cytotoxic activity against human H1299 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
Cytotoxic activity against human H1299 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
[PMID: 27156773]
OVCAR-8 IC50
72 μM
Compound: 1; EA
Antiproliferative activity against human OVCAR8 cells after 24 to 72 hrs by MTS assay
Antiproliferative activity against human OVCAR8 cells after 24 to 72 hrs by MTS assay
[PMID: 27448922]
PC-3 IC50
75 μM
Compound: 1; EA
Antiproliferative activity against human PC3 cells after 24 to 72 hrs by MTS assay
Antiproliferative activity against human PC3 cells after 24 to 72 hrs by MTS assay
[PMID: 27448922]
SF-188 IC50
31.65 μM
Compound: EA
Cytotoxic activity against human SF188 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
Cytotoxic activity against human SF188 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
[PMID: 27156773]
SK-BR-3 IC50
34.21 μM
Compound: EA
Cytotoxic activity against human SKBR3 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
Cytotoxic activity against human SKBR3 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
[PMID: 27156773]
SK-OV-3 IC50
> 100 μM
Compound: 1; EA
Antiproliferative activity against human SKOV3 cells after 24 to 72 hrs by MTS assay
Antiproliferative activity against human SKOV3 cells after 24 to 72 hrs by MTS assay
[PMID: 27448922]
SW480 IC50
32.7 μM
Compound: 1
Inhibition of Wnt/beta-casein signaling in human SW480 cells by fluorimetry
Inhibition of Wnt/beta-casein signaling in human SW480 cells by fluorimetry
[PMID: 19121941]
体外研究
(In Vitro)

Ethacrynic acid (50 μM; 24 小时) 抑制 CLL 细胞中 Wnt/β-catenin 的信号传导[1]
Ethacrynic acid (1-100 μM; 48 小时) 在 CLL 细胞中具有细胞毒性,IC50 为 8.56 μM[1]
Ethacrynic acid (0.01-0.25 mmol/L; 30 分钟) 增加眼睛的房水流出,出水率由28%提高到105%[2]
Ethacrynic acid (10-100 μM; 30 分钟) 在 LPS (100 ng/mL) 诱导的 RAW264.7 细胞中能够抑制 NF-κB 通路的激活,具有抗炎活性[3]
Ethacrynic acid (20 μM/mL; 2 小时) 可以增强经辐射照射后的 MCF-7 癌细胞中的辐射强度[3]
Ethacrynic acid (100 μmol/L; 62.5-250分钟) 以剂量依赖性的方式抑制高 –K+ (80 mmol/L) 和乙酰胆碱 (acetylcholine, ACh, 100 µmol/L) 引起的小鼠气管环收缩,EC50 分别为 40.28 µmol/L 和 56.22 µmol/L[8]
Ethacrynic acid (100 μmol/L; 500-2500 秒) 分别降低高 –K+ 和 ACh 诱导的细胞内 Ca2+ 浓度,分别从 0.40 降到 0.16,0.50 降到 0.39 [8]

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

RT-PCR[1]

Cell Line: Chronic lymphocytic leukemia (CLL)
Concentration: 1 μM, 10 μM, 100 μM
Incubation Time: 16 h
Result: Depressed the expression of LEF-1, Cyclin D1 and Fibronectin in a concentration-dependent manner.( LEF-1, cyclin D1 and fibronectin are established target genes of the Wnt/b-catenin pathway).

Western Blot Analysis[3]

Cell Line: RAW 264.7
Concentration: 10 μM, 20 μM, 50 μM, 100 μM ;Before LPS treatment (100 ng/mL; 1 h)
Incubation Time: 30 min
Result: Inhibited the expression of iNOS mRNA.
Inhibited degradation of IκBα and IκBβ.
体内研究
(In Vivo)

Ethacrynic acid (450 μg/mouse; 口服给药; 一天一次连续60天) 能够抑制小鼠中的胞瘤生长[5]

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

Animal Model: Myeloma Balb/c mice model[5]
Dosage: 450 μg/mouse
Administration: Oral gavage (p.o.); Once daily for 60 days. After BALB/c mice were injected subcutaneously with 5 × 105 MPC11 myeloma cells.
Result: Significantly inhibited tumor growth.
Clinical Trial
分子量

303.14

Formula

C13H12Cl2O4

CAS 号
性状

固体

颜色

White to off-white

中文名称

依他尼酸; 利尿酸

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, 1 year; -20°C, 6 months (protect from light)

溶解性数据
细胞实验: 

DMSO 中的溶解度 : 100 mg/mL (329.88 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

H2O 中的溶解度 : 27.5 mg/mL (90.72 mM; 超声助溶)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.2988 mL 16.4940 mL 32.9881 mL
5 mM 0.6598 mL 3.2988 mL 6.5976 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, 1 year; -20°C, 6 months (protect from light)。-80°C储存时,请在1年内使用, -20°C储存时,请在6个月内使用。

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

  • 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

动物实验:

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (8.25 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (8.25 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

    2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。

以下溶解方案,请直接配制工作液。建议现用现配,在短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比; 如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶。

  • 方案 一

    请依序添加每种溶剂: PBS

    Solubility: 1 mg/mL (3.30 mM); 澄清溶液; 超声助溶

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
该产品水溶性佳,请具体参考实测 水 / PBS / Saline 中的溶解度数据。
您所需的储备液浓度超过该产品的实测溶解度,如有需要,请与 MCE 中国技术支持联系。
纯度 & 产品资料

纯度: 99.98%

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, 1 year; -20°C, 6 months (protect from light)。-80°C储存时,请在1年内使用, -20°C储存时,请在6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
H2O / DMSO 1 mM 3.2988 mL 16.4940 mL 32.9881 mL 82.4701 mL
5 mM 0.6598 mL 3.2988 mL 6.5976 mL 16.4940 mL
10 mM 0.3299 mL 1.6494 mL 3.2988 mL 8.2470 mL
15 mM 0.2199 mL 1.0996 mL 2.1992 mL 5.4980 mL
20 mM 0.1649 mL 0.8247 mL 1.6494 mL 4.1235 mL
25 mM 0.1320 mL 0.6598 mL 1.3195 mL 3.2988 mL
30 mM 0.1100 mL 0.5498 mL 1.0996 mL 2.7490 mL
40 mM 0.0825 mL 0.4124 mL 0.8247 mL 2.0618 mL
50 mM 0.0660 mL 0.3299 mL 0.6598 mL 1.6494 mL
60 mM 0.0550 mL 0.2749 mL 0.5498 mL 1.3745 mL
80 mM 0.0412 mL 0.2062 mL 0.4124 mL 1.0309 mL
DMSO 100 mM 0.0330 mL 0.1649 mL 0.3299 mL 0.8247 mL

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

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:
Ethacrynic acid
目录号:
HY-B1640
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