MSC-4381

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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。

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. 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.

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Animal Model:MC38 tumor-bearing C57/BL6 miceDosage: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 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.

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Membrane Transporter/Ion Channel

Monocarboxylate Transporter

Monocarboxylate transporter

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2445185-57-7

537.97

C26H20ClN3O6S

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 83.33 mg/mL (154.90 mM; 超声助溶 (<60°C)

CCOc1ccc(c2ncccc12)S(=O)(=O)Nc1ccc(Cl)cc1C#Cc1cnc(cc1OC)C(O)=O

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(-20℃)

With Ice Pack

≥ 2 years