1. Membrane Transporter/Ion Channel
  2. Monocarboxylate Transporter
  3. α-Cyano-4-hydroxycinnamic acid

α-Cyano-4-hydroxycinnamic acid  (Synonyms: α-Cyano-4-hydroxycinnamate)

目录号: HY-107641 纯度: 99.98%
COA 产品使用指南

α-Cyano-4-hydroxycinnamic acid (α-Cyano-4-hydroxycinnamate) 是有效的非竞争性单羧酸盐转运蛋白 (MCTs) 抑制剂。α-Cyano-4-hydroxycinnamic acid 抑制线粒体丙酮酸转运蛋白,Ki 值为 6.3 μM。α-Cyano-4-hydroxycinnamic acid 用作基质辅助激光解吸电离-飞行时间质谱 (MALDI-TOF) 分析的基质,可以促进肽离子化。

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α-Cyano-4-hydroxycinnamic acid Chemical Structure

α-Cyano-4-hydroxycinnamic acid Chemical Structure

CAS No. : 28166-41-8

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10 mM * 1 mL in DMSO ¥550
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50 mg ¥391
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100 mg ¥548
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查看 Monocarboxylate Transporter 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

α-Cyano-4-hydroxycinnamic acid (α-Cyano-4-hydroxycinnamate) is a potent and non-competitive inhibitor of monocarboxylate transporters (MCTs). α-Cyano-4-hydroxycinnamic acid inhibits mitochondrial pyruvate transporter with a Ki of 6.3 μM. α-Cyano-4-hydroxycinnamic acid is used as a matrix to facilitate peptide ionization in matrix-assisted laser desorption/ionization time-of-flight (MALDI-TOF) mass spectrometry applications[1][2].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HCT-116 IC50
1650 μM
Compound: CHC
Cytotoxicity against human HCT-116 cells overexpressing MCT-1 assessed as reduction in cell viability measured after 72 hrs by MTT assay
Cytotoxicity against human HCT-116 cells overexpressing MCT-1 assessed as reduction in cell viability measured after 72 hrs by MTT assay
[PMID: 33221062]
HeLa IC50
2140 μM
Compound: CHC
Cytotoxicity against human HeLa cells overexpressing MCT-1 assessed as reduction in cell viability measured after 72 hrs by MTT assay
Cytotoxicity against human HeLa cells overexpressing MCT-1 assessed as reduction in cell viability measured after 72 hrs by MTT assay
[PMID: 33221062]
HT-29 IC50
30.4 μM
Compound: CHCA
Desensitization of GPR35 receptor in human HT-29 cells assessed as inhibition of zaprinast-induced dynamic mass redistribution after 10 mins
Desensitization of GPR35 receptor in human HT-29 cells assessed as inhibition of zaprinast-induced dynamic mass redistribution after 10 mins
[PMID: 24900447]
HT-29 EC50
9.8 μM
Compound: CHCA
Agonist activity at GPR35 receptor in human HT-29 cells after 10 mins by dynamic mass redistribution assay
Agonist activity at GPR35 receptor in human HT-29 cells after 10 mins by dynamic mass redistribution assay
[PMID: 24900447]
SiHa IC50
10.7 μM
Compound: CHC
Inhibition of MCT4-mediated [14C]-lactate uptake in human SiHa cells in lactate-containing medium assessed as remaining lactate concentration in culture medium after 12 mins by liquid scintillation counting
Inhibition of MCT4-mediated [14C]-lactate uptake in human SiHa cells in lactate-containing medium assessed as remaining lactate concentration in culture medium after 12 mins by liquid scintillation counting
[PMID: 24095010]
SiHa EC50
10.7 μM
Compound: CHC
Cytotoxicity against human SiHa cells in lactate-containing medium after 72 hrs by MTT assay
Cytotoxicity against human SiHa cells in lactate-containing medium after 72 hrs by MTT assay
[PMID: 24095010]
SiHa IC50
43.5 μM
Compound: CHC
Inhibition of MCT4-mediated [14C]-lactate uptake in human SiHa cells in lactate-containing medium assessed as remaining lactate concentration in culture medium after 24 hrs by liquid scintillation counting
Inhibition of MCT4-mediated [14C]-lactate uptake in human SiHa cells in lactate-containing medium assessed as remaining lactate concentration in culture medium after 24 hrs by liquid scintillation counting
[PMID: 24095010]
U2OS EC50
70.7 μM
Compound: CHCA
Agonist activity at GPR35 receptor in human U2OS cells coexpressing Gal4-VP16-TEV assessed as beta arrestin translocation after 5 hrs by beta lactamase reporter gene assay
Agonist activity at GPR35 receptor in human U2OS cells coexpressing Gal4-VP16-TEV assessed as beta arrestin translocation after 5 hrs by beta lactamase reporter gene assay
[PMID: 24900447]
体外研究
(In Vitro)

α-Cyano-4-hydroxycinnamic acid (α-Cyano-4-hydroxycinnamate) inhibits monocarboxylates transport such as lactate and pyruvate[2].
? α-Cyano-4-hydroxycinnamic acid (CHC; 0.5 mM and 1 mM) of 1 mM has a significant inhibitory effect on branching morphogenesis and decreases the epithelial perimeter and area of lung explants in a dose dependent way[2].
? At 100 μM concentration, α-Cyano-4-hydroxycinnamic acid rapidly and almost totally inhibits O2 uptake by rat heart mitochondria oxidizing pyruvate. Inhibition can be detected at concentrations of inhibitor as low as 1 μM although inhibition took time to develop at this concentration[1].

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

分子量

189.17

Formula

C10H7NO3

CAS 号
性状

固体

颜色

Light yellow to yellow

中文名称

α-氰基-4-羟基肉桂酸

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
细胞实验: 

DMSO 中的溶解度 : 250 mg/mL (1321.56 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 : < 0.1 mg/mL (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 5.2863 mL 26.4313 mL 52.8625 mL
5 mM 1.0573 mL 5.2863 mL 10.5725 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: ≥ 2.08 mg/mL (11.00 mM); 澄清溶液

    此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 20.8 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: ≥ 2.08 mg/mL (11.00 mM); 澄清溶液

    此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 20.8 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。
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
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
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, 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 5.2863 mL 26.4313 mL 52.8625 mL 132.1563 mL
5 mM 1.0573 mL 5.2863 mL 10.5725 mL 26.4313 mL
10 mM 0.5286 mL 2.6431 mL 5.2863 mL 13.2156 mL
15 mM 0.3524 mL 1.7621 mL 3.5242 mL 8.8104 mL
20 mM 0.2643 mL 1.3216 mL 2.6431 mL 6.6078 mL
25 mM 0.2115 mL 1.0573 mL 2.1145 mL 5.2863 mL
30 mM 0.1762 mL 0.8810 mL 1.7621 mL 4.4052 mL
40 mM 0.1322 mL 0.6608 mL 1.3216 mL 3.3039 mL
50 mM 0.1057 mL 0.5286 mL 1.0573 mL 2.6431 mL
60 mM 0.0881 mL 0.4405 mL 0.8810 mL 2.2026 mL
80 mM 0.0661 mL 0.3304 mL 0.6608 mL 1.6520 mL
100 mM 0.0529 mL 0.2643 mL 0.5286 mL 1.3216 mL
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    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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α-Cyano-4-hydroxycinnamic acid
目录号:
HY-107641
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