|(S)-6-[(3,5-二甲基-1H-吡唑-4-基)甲基]-5-[(4-羟基异唑烷-2-基)羰基]-1-异丁基-3-甲基噻吩并[2,3-d]嘧啶-2,4(1H,3H)-二酮|CsnPharm

CAS No.: 496791-37-8

AR-C155858 Catalog No. CSN15986

Synonyms: AR-C155858

AR-C155858 is an inhibitor of the monocarboxylate transporters (MCTs) MCT1 and MCT2 (Ki values are 2.3 and < 10 nM, respectively), and exhibits no activity at MCT4.

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400-920-2911

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述AR-C155858 is a potent inhibitor of both MCT1 and MCT2 with Ki values of 2.3 and <10nM, respectively. AR-C155858 at concentration ranging in 10-100nM dose-dependently decreased the rate of L-lactate uptake in separate oocytes. AR-C155858 at concentration of 100nM potently blocked Raji cell proliferation after 3 days. Immediate increases in the levels of intracellular lactate and a block in lactate export within 8 hours can be observed by MCT1 inhibition through 100nM AR-C155858.
动物研究
剂量
Mice: 5 mg/kg^[3] (i.v.), 0.1 mg/kg^[1] (i.v.); 10 mg/kg^[4] (i.p.)

给药途径
i.v., i.p.
参考文献

动物研究
剂量	Mice: 5 mg/kg^[3] (i.v.), 0.1 mg/kg^[1] (i.v.); 10 mg/kg^[4] (i.p.)
给药途径	i.v., i.p.

[1] Vijay N, Morse BL, 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.
[2] Ovens MJ, Manoharan C, 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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1667 mL
- 10.8334 mL
- 21.6668 mL
- 5 mM
- 0.4333 mL
- 2.1667 mL
- 4.3334 mL
- 10 mM
- 0.2167 mL
- 1.0833 mL
- 2.1667 mL

技术信息

CAS号

496791-37-8

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C21H27N5O5S

运输

蓝冰

分子量

461.53

别名

AR-C155858

溶解度

DMSO	170.0 mg/mL (368.3 mM)
Water	9.67 mg/mL (20.9 mM)

动物实验配方

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