Mivotilate (YH439)
(Synonyms: YH439) 目录号 : GC30297
Mivotilate (YH439) 是一种无毒、有效的芳烃受体 (AhR) 激活剂，可作为保肝剂。
Cas No.:130112-42-4
Sample solution is provided at 25 µL, 10mM.
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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.
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. | |
| Cas No. | 130112-42-4 | SDF | |
| 别名 | YH439 | ||
| Canonical SMILES | O=C(OC(C)C)/C(C(NC1=NC(C)=CS1)=O)=C2SCS\2 | ||
| 分子式 | C12H14N2O3S3 | 分子量 | 330.45 |
| 溶解度 | DMSO : 12.5 mg/mL (37.83 mM; ultrasonic and warming and heat to 60°C) | 储存条件 | 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℃，然后在超声波浴中震荡一段时间。 |
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| 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。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.0262 mL | 15.1309 mL | 30.2618 mL |
| 5 mM | 0.6052 mL | 3.0262 mL | 6.0524 mL |
| 10 mM | 0.3026 mL | 1.5131 mL | 3.0262 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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