MCT4-IN-1 - CAS:2445185-57-7

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MCT4-IN-1

目录号 : KM8904 CAS No. : 2445185-57-7 纯度 : 98%

Data Sheet 产品使用指南

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，K_i 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。

规格	价格	是否有货
5mg		In-stock
10mg		In-stock
50mg	询价	In-stock
100mg	询价	In-stock

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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 K_i 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.

体外研究

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 K_i of 11 nM by fluorescence cross-correlation spectroscopy (FCCS).
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.

体内研究

MCT4-IN-1 (compound 18n; 30 mg/kg; PO; single dose) only combined with MCT1/2 inhibitor exhibits a significant tumoral intracellular lactate accumulation.
MCT4-IN-1 (30 mg/kg/day; for 15 days) shows no significant antitumor activity.
MCT4-IN-1 (0.2 mg/kg; iv) has a T_1/2 of 1 hours, a CL of 0.33 L/h•kg, a C_max of 489 ng/mL and a V_ss of 0.4 L/kg for mice.

Animal Model:	MC38 tumor-bearing C57/BL6 mice
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
Dosage:	0.2 mg/kg (Pharmacokinetic Analysis)
Administration:	IV
Result:	Had a T_1/2 of 1 hours, a CL of 0.33 L/h•kg, a C_max of 489 ng/mL and a V_ss of 0.4 L/kg for mice.

分子式

C₂₆H₂₀ClN₃O₆S

分子量

537.97

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

纯度： 98%

Data Sheet

产品使用指南

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

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第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

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工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系客服）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

配置后的溶液总体积：

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

Other Forms of Rapamycin:

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The molarity calculator equation

The dilution calculator equation

动物实验计算换算器