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AR-C155858

AR-C155858 是单羧酸转运蛋白 MCT1 和 MCT2 的抑制剂，Ki 分别为2.3和 10 nM。

CAS号

496791-37-8

分子式

C21H27N5O5S

主要靶点

Monocarboxylate transporter

仅限科研使用

Cat No : CM05031

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Synonyms

验证数据展示

  • CAS No.: 496791-37-8

    AR-C155858
    CAS#: 496791-37-8

产品信息

AR-C155858 is an inhibitor of monocarboxylate transporter MCT1 and MCT2 (Kis: 2.3 nM and 10 nM).

CAS号 496791-37-8
分子式 C21H27N5O5S
主要靶点 Monocarboxylate transporter
主要通路 离子通道
分子量 461.54
纯度 98.84%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名

靶点活性

MCT2:10 nM(ki)|MCT1:(ki)2.3 nM

体外活性

AR-C155858 (10 nM-100 nM) inhibits MCT1/MCT2 C-terminal chimaeras[1]. AR-C155858 inhibits MCT1 expressed in Xenopus oocytes in a time- and concentration-dependent manner[2]. AR-C155858 inhibits MCT2, and the 70% inhibition seen at 10 nM is followed by a gradually increasing inhibition which can only be explained by a Ki value of significantly less than 10 nM.

溶解度

DMSO:40 mg/mL (86.67 mM)

参考文献

1.Ovens MJ, et al. The inhibition of monocarboxylate transporter 2 (MCT2) by AR-C155858 is modulated by the associated ancillary protein. Biochem J. 2010 Oct 15;431(2):217-25.
2.Ovens MJ, et al. AR-C155858 is a potent inhibitor of monocarboxylate transporters MCT1 and MCT2 that binds to an intracellular site involving transmembrane helices 7-10. Biochem J. 2010 Jan 15;425(3):523-30.
3.Vijay N, et al. A Novel Monocarboxylate Transporter Inhibitor as a Potential Treatment Strategy for γ-Hydroxybutyric Acid Overdose. Pharm Res. 2015 Jun;32(6):1894-906.

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