MCT4-IN-1

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

MCT4-IN-1  纯度: 98.11%

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。MCT4-IN-1 靶向与 MCT4 的胞质域。MCT4-IN-1 导致高表达 MCT4 细胞中乳酸流出的抑制和细胞活力的降低。MCT4-IN-1 具有用于 MCT4 转运蛋白研究的潜力。

MCT4-IN-1

MCT4-IN-1 Chemical Structure

CAS No. : 2445185-57-7

规格 价格 是否有货 数量
5 mg ￥5100 In-stock
10 mg ￥8200 In-stock
50 mg   询价  
100 mg   询价  

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MCT4-IN-1 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Membrane Transporter/Ion Channel Compound Library
  • Anti-Cancer Compound Library
  • Orally Active Compound Library
  • Anti-Cancer Metabolism Compound Library

生物活性

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. MCT4-IN-1 targets to the cytosolic domain of MCT4. MCT4-IN-1 results in lactate efflux inhibition and reduction of cellular viability in MCT4 high expressing cells. MCT4-IN-1 has the potential for MCT4 transporter inhibition research[1].

体外研究
(In Vitro)

MCT4-IN-1 (compound 18n) inhibits lactate efflux in the MDA-MB-231 cell line with an IC50 of 1 nM. The on-target activity is confirmed with a Ki of 11 nM by fluorescence cross-correlation spectroscopy (FCCS)[1].
MCT4-IN-1 does not inhibit lactate efflux to a similar extent in SNU-398 and MiaPaca2, and only 600-fold less in RT-4 cell lines[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

MCT4-IN-1 (compound 18n; 30 mg/kg; PO; single dose) only combined with MCT1/2 inhibitor exhibits a significant tumoral intracellular lactate accumulation[1].
MCT4-IN-1 (30 mg/kg/day; for 15 days) shows no significant antitumor activity[1].
MCT4-IN-1 (0.2 mg/kg; iv) has 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[1].

上海金畔生物科技有限公司 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

2445185-57-7
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 : 83.33 mg/mL (154.90 mM; ultrasonic and warming and heat to 60°C)

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
10 mM 0.1859 mL 0.9294 mL 1.8588 mL

*

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。

In Vivo:

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

  • 1.

    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); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.87 mM，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；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Timo Heinrich, et al. Discovery of 5-{2-[5-Chloro-2-(5-ethoxyquinoline-8-sulfonamido)phenyl]ethynyl}-4-methoxypyridine-2-carboxylic Acid, a Highly Selective in Vivo Useable Chemical Probe to Dissect MCT4 Biology. J Med Chem. 2021 Aug 26;64(16):11904-11933.

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