MSC-4381 MCT4-IN-1|cas:2445185-57-7|西域试剂

MSC-4381 MCT4-IN-1,98.11%

产品编号：Bellancom-132301| CAS NO：2445185-57-7| 分子式：C₂₆H₂₀ClN₃O₆S| 分子量：537.97

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	包装	价格	库存与货期	购买量	操作
Bellancom-132301		￥5100.00	杭州北京（现货）
Bellancom-132301		￥8200.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

MSC-4381 MCT4-IN-1

产品介绍

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，K_i 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。

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 K_i 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.

体外研究

MSC-4381 (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).
MSC-4381 does not inhibit lactate efflux to a similar extent in SNU-398 and MiaPaca2, and only 600-fold less in RT-4 cell lines.

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

体内研究

MSC-4381 (compound 18n; 30 mg/kg; PO; single dose) only combined with MCT1/2 inhibitor exhibits a significant tumoral intracellular lactate accumulation.
MSC-4381 (30 mg/kg/day; for 15 days) shows no significant antitumor activity.
MSC-4381 (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.

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

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.

体内研究

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

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.

性状

Solid

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