GlpBio

Mivotilate (YH439)

目录号: GC30297纯度: >98.00%同义词: YH439
Mivotilate (YH439) 是一种无毒、有效的芳烃受体 (AhR) 激活剂，可作为保肝剂。
Mivotilate (YH439)
Cas No.: 130112-42-4
规格价格库存数量操作
1mg¥900.00现货
1
5mg¥2,700.00现货
1
10mg¥4,320.00现货
1
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产品描述 Description

Mivotilate is a nontoxic, potent activator of the aryl hydrocarbon receptor (AhR), and acts as a hepatoprotective agent.

Mivotilate is a nontoxic, potent activator of the aryl hydrocarbon receptor. Mivotilate (YH439) has a novel activation mode that tolerates mutation of histidine 285 to tyrosine[1]. Mivotilate induces cytochromes P4501A1/2 (CYP1A1/2) through the aryl hydrocarbon (Ah) receptor[3].

Mivotilate (YH439, 150 mg/kg, p.o.) reduces CYP2E1-mediated NDMA demethylase activity in rats, but shows no obvious effect on NADPH-dependent P450 oxidoreductase activity. Mivotilate (75-300 mg/kg) rapidly decreases immunoreactive CYP2E1 protein. Mivotilate (150 mg/kg, p.o.) inhibits the transcription of CYP2E1 in rats[2].

[1]. Whelan F, et al. Amino acid substitutions in the aryl hydrocarbon receptor ligand binding domain reveal YH439 as an atypical AhR activator. Mol Pharmacol. 2010 Jun;77(6):1037-46. [2]. Jeong KS, et al. Transcriptional inhibition of cytochrome P4502E1 by a synthetic compound, YH439. Arch Biochem Biophys. 1996 Feb 1;326(1):137-44. [3]. Lee IJ, et al. Transcriptional induction of the cytochrome P4501A1 gene by a thiazolium compound, YH439. Mol Pharmacol. 1996 Jun;49(6):980-8.

实验参考方法 Experimental Reference Method

Animal experiment:

Male outbred Sprague-Dawley rats (weighing 100-150 g) are kept on a 12-h light-dark cycle with NIH 31 autoclavable rat die and water ad libitum. After a single oral administration of Mivotilate (75, 150, and 300 mg/kg body wt, diluted in corn oil), the animals are sacrificed at different times as indicated. Livers from control (corn oil-treated), starved (2 days) and Mivotilate-treated animals (n = 5 per group) are immediately excised, freeze-clamped, and processed further. Another group of rats (n = 3) is treated with phenobarbital (100 mg/kg/day) by intraperitoneal injection for 2 days and sacrificed 24 h after the last dose[2].

References:

[1]. Whelan F, et al. Amino acid substitutions in the aryl hydrocarbon receptor ligand binding domain reveal YH439 as an atypical AhR activator. Mol Pharmacol. 2010 Jun;77(6):1037-46.
[2]. Jeong KS, et al. Transcriptional inhibition of cytochrome P4502E1 by a synthetic compound, YH439. Arch Biochem Biophys. 1996 Feb 1;326(1):137-44.
[3]. Lee IJ, et al. Transcriptional induction of the cytochrome P4501A1 gene by a thiazolium compound, YH439. Mol Pharmacol. 1996 Jun;49(6):980-8.

产品文档 Product Documents

Purity:>98.00%

化学性质Chemical Properties

CAS 号
130112-42-4
同义词
YH439
SMILES
O=C(OC(C)C)/C(C(NC1=NC(C)=CS1)=O)=C2SCS\2
分子式
C12H14N2O3S3
分子量
330.45 g/mol
溶解性
DMSO : 12.5 mg/mL (37.83 mM; ultrasonic and warming and heat to 60°C)
保存条件
Store at -20°C
General tips
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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol