Pyributicarb (TSH-888)
(Synonyms: 稗草畏,TSH-888) 目录号 : GC33862
Pyributicarb (TSH-888) 是一种氨基甲酸酯类除草剂，是 CYP3A4 基因和人孕烷 X 受体 (hPXR) 的有效激活剂。
Cas No.:88678-67-5
Sample solution is provided at 25 µL, 10mM.
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Pyributicarb, a carbamate-type herbicide, is a potent activator of both CYP3A4 gene and human pregnane X receptor (hPXR).
Pyributicarb, a carbamate-type herbicide, is a potent activator of both CYP3A4 gene and human pregnane X receptor (hPXR). Pyributicarb is found to increase the CYP3A4 reporter activity at 0.1 to 1 μM more strongly than typical CYP3A4 inducer rifampicin. Expression of hPXR-siRNA clearly diminishes the Pyributicarb-stimulated CYP3A4 reporter activity in 3-1-10 cells and decreases the endogenous CYP3A4 mRNA levels in HepG2 cells[1]. Pyributicarb induces luciferase transcription via hPXR at low concentrations in the order of 10 nM. The relative potency of Pyributicarb for hPXR is 8.6-fold that of rifampicin (RIF)[2].
Pyributicarb causes enhancement of CYP3A4-derived reporter activity in mouse livers introduced with hPXR by adenovirus[1].
[1]. Matsubara T, et al. Assessment of human pregnane X receptor involvement in pesticide-mediated activation of CYP3A4 gene. Drug Metab Dispos. 2007 May;35(5):728-33. [2]. Kojima H, et al. Comparative study of human and mouse pregnane X receptor agonistic activity in 200 pesticides using in vitro reporter gene assays. Toxicology. 2011 Feb 27;280(3):77-87.
Cell experiment: | HepG2-derived cells stably expressing the CYP3A4 reporter gene (3-1-10 cells) are used in this experiment. The cells are treated with 0.3 to 30 μM Pyributicarb for 48 h. Then reporter activities are determined[1]. |
Animal experiment: | Male ICR mice (5 weeks old) are used and fed standard rodent chow. After 18-h fasting, mice are injected i.v. with adenovirus [4.0 ×109 50% titer culture infectious dose (TCID50)/mouse]. Three days after the infection, vehicle (0.5% methyl cellulose/saline) or Pyributicarb (100 mg/kg/day) is administered p.o. for 2 consecutive days. Animals are killed 20 h after the last dose[1]. |
References: [1]. Matsubara T, et al. Assessment of human pregnane X receptor involvement in pesticide-mediated activation of CYP3A4 gene. Drug Metab Dispos. 2007 May;35(5):728-33. | |
| Cas No. | 88678-67-5 | SDF | |
| 别名 | 稗草畏,TSH-888 | ||
| Canonical SMILES | S=C(OC1=CC=CC(C(C)(C)C)=C1)N(C2=NC(OC)=CC=C2)C | ||
| 分子式 | C18H22N2O2S | 分子量 | 330.44 |
| 溶解度 | DMSO : 100 mg/mL (302.63 mM);Water : < 0.1 mg/mL (insoluble) | 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 | 3.0263 mL | 15.1313 mL | 30.2627 mL |
| 5 mM | 0.6053 mL | 3.0263 mL | 6.0525 mL |
| 10 mM | 0.3026 mL | 1.5131 mL | 3.0263 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
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet