2. Membrane Transporter/Ion Channel
  3. Monocarboxylate Transporter
  4. MSC-4381

MSC-4381  (Synonyms: MCT4-IN-1)

目录号: HY-132301 纯度: 98.89%
COA 产品使用指南

摩尔计算器

MSC-4381 (MCT4-IN-1) 是一种口服有效的，选择性的单羧酸转运蛋白 4 (MCT4/SLC16A3) 抑制剂，IC50 值为 77 nM，Ki 值为 11 nM。MSC-4381 靶向与 MCT4 的胞质域。MSC-4381 导致高表达 MCT4 细胞中乳酸流出的抑制和细胞活力的降低。MSC-4381 具有用于 MCT4 转运蛋白研究的潜力。

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MSC-4381 Chemical Structure

MSC-4381 Chemical Structure

CAS No. : 2445185-57-7

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1184
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1 mg ￥500
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5 mg ￥1000
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10 mg ￥1400
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25 mg ￥2500
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50 mg ￥4300
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MSC-4381 相关抗体

Top Publications Citing Use of Products

查看 Monocarboxylate Transporter 亚型特异性产品:

查看所有亚型
MCT1 MCT2 MCT4

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MSC-4381 (MCT4-IN-1) is an orally active and selective monocarboxylate transporter 4 (MCT4/SLC16A3) inhibitor with an IC50 of 77 nM and a Ki of 11 nM. MSC-4381 targets to the cytosolic domain of MCT4. MSC-4381 results in lactate efflux inhibition and reduction of cellular viability in MCT4 high expressing cells. MSC-4381 has the potential for MCT4 transporter inhibition research[1]. MSC-4381 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

IC50 & Target

MCT4

77 nM (IC50)

MCT4

11 nM (Ki)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
MDA-MB-231 IC50
1 nM
Compound: 18n
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in intracellular lactate accumulation preincubated for 30 mins followed by D(+)glucose and measured after 4 hrs by UHPLC-ESI-Q-Orbitrap-MS analysis
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in intracellular lactate accumulation preincubated for 30 mins followed by D(+)glucose and measured after 4 hrs by UHPLC-ESI-Q-Orbitrap-MS analysis
[PMID: 34382802]
MDA-MB-231 IC50
11 nM
Compound: 18n
Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 6 days by MTS assay
Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 6 days by MTS assay
[PMID: 34382802]
MIA PaCa-2 IC50
> 25000 nM
Compound: 18n
Cytotoxicity against human MIA PaCa-2 cells assessed as reduction in intracellular lactate accumulation preincubated for 30 mins followed by D(+)glucose and measured after 4 hrs by UHPLC-ESI-Q-Orbitrap-MS analysis
Cytotoxicity against human MIA PaCa-2 cells assessed as reduction in intracellular lactate accumulation preincubated for 30 mins followed by D(+)glucose and measured after 4 hrs by UHPLC-ESI-Q-Orbitrap-MS analysis
[PMID: 34382802]
MIA PaCa-2 IC50
4720 nM
Compound: 18n
Cytotoxicity against human MIA PaCa-2 cells assessed as inhibition of cell growth incubated for 6 days by MTS assay
Cytotoxicity against human MIA PaCa-2 cells assessed as inhibition of cell growth incubated for 6 days by MTS assay
[PMID: 34382802]
NCI-H358 IC50
3 nM
Compound: 18n
Cytotoxicity against human NCI-H358 cells assessed as reduction in intracellular lactate accumulation preincubated for 30 mins followed by D(+)glucose and measured after 4 hrs by UHPLC-ESI-Q-Orbitrap-MS analysis
Cytotoxicity against human NCI-H358 cells assessed as reduction in intracellular lactate accumulation preincubated for 30 mins followed by D(+)glucose and measured after 4 hrs by UHPLC-ESI-Q-Orbitrap-MS analysis
[PMID: 34382802]
RT-4 IC50
638 nM
Compound: 18n
Cytotoxicity against human RT-4 cells assessed as reduction in intracellular lactate accumulation preincubated for 30 mins followed by D(+)glucose and measured after 4 hrs by UHPLC-ESI-Q-Orbitrap-MS analysis
Cytotoxicity against human RT-4 cells assessed as reduction in intracellular lactate accumulation preincubated for 30 mins followed by D(+)glucose and measured after 4 hrs by UHPLC-ESI-Q-Orbitrap-MS analysis
[PMID: 34382802]
SNU-398 IC50
> 25000 nM
Compound: 18n
Cytotoxicity against human SNU-398 cells assessed as reduction in intracellular lactate accumulation preincubated for 30 mins followed by D(+)glucose and measured after 4 hrs by UHPLC-ESI-Q-Orbitrap-MS analysis
Cytotoxicity against human SNU-398 cells assessed as reduction in intracellular lactate accumulation preincubated for 30 mins followed by D(+)glucose and measured after 4 hrs by UHPLC-ESI-Q-Orbitrap-MS analysis
[PMID: 34382802]
体外研究
(In Vitro)

MSC-4381 (化合物 18n) 抑制 MDA-MB-231 细胞系中的乳酸流出，IC50 为 1 nM。通过荧光互相关光谱 (FCCS) 确认了靶向活性，Ki 为 11 nM[1]。
MSC-4381 在 SNU-398 和 MiaPaca2 中对乳酸流出的抑制程度相似，在 RT-4 细胞系中仅低 600 倍[1]。

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

MSC-4381 相关抗体:
体内研究
(In Vivo)

MSC-4381 (化合物 18n；30 mg/kg；口服单剂量) 仅与 MCT1/2 抑制剂联合使用时表现出显著的肿瘤细胞内乳酸积累[1]。
MSC-4381 (30 mg/kg/天；持续 15 天) 未显示出显著的抗肿瘤活性[1]。
MSC-4381 (0.2 mg/kg；iv) 的 T1/2 为 1 小时，CL 为 0.33 L/h kg，Cmax 为 489 ng/mL，小鼠的 Vss 为 0.4 L/kg[1]。

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

Animal Model: MC38 tumor-bearing C57/BL6 mice[1]
Dosage: 30 mg/kg
Administration: PO; single dose
Result: Only combined with MCT1/2 inhibitor exhibited a significant tumoral intracellular lactate accumulation.
Animal Model: Mice[1]
Dosage: 0.2 mg/kg (Pharmacokinetic Analysis)
Administration: IV
Result: Had a T1/2 of 1 hours, a CL of 0.33 L/h•kg, a Cmax of 489 ng/mL and a Vss of 0.4 L/kg for mice.
分子量

537.97

Formula

C26H20ClN3O6S
CAS 号
性状

固体

颜色

White to yellow

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 : 83.33 mg/mL (154.90 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 1.8588 mL 9.2942 mL 18.5884 mL
5 mM 0.3718 mL 1.8588 mL 3.7177 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 (3.87 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。

    以 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。
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
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
参考文献

MSC-4381 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 1.8588 mL 9.2942 mL 18.5884 mL 46.4710 mL
5 mM 0.3718 mL 1.8588 mL 3.7177 mL 9.2942 mL
10 mM 0.1859 mL 0.9294 mL 1.8588 mL 4.6471 mL
15 mM 0.1239 mL 0.6196 mL 1.2392 mL 3.0981 mL
20 mM 0.0929 mL 0.4647 mL 0.9294 mL 2.3235 mL
25 mM 0.0744 mL 0.3718 mL 0.7435 mL 1.8588 mL
30 mM 0.0620 mL 0.3098 mL 0.6196 mL 1.5490 mL
40 mM 0.0465 mL 0.2324 mL 0.4647 mL 1.1618 mL
50 mM 0.0372 mL 0.1859 mL 0.3718 mL 0.9294 mL
60 mM 0.0310 mL 0.1549 mL 0.3098 mL 0.7745 mL
80 mM 0.0232 mL 0.1162 mL 0.2324 mL 0.5809 mL
100 mM 0.0186 mL 0.0929 mL 0.1859 mL 0.4647 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:

MSC-43812445185-57-7MCT4-IN-1MSC4381MSC 4381Monocarboxylate TransporterorallyMCT4SLC16A3cytosoliclactateeffluxMDA-MB-231SNU-398MiaPaca2Inhibitorinhibitorinhibit

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