| CAS |
No.88678-67-5 |
| 中文名称 |
稗草畏 |
| 英文名称 |
Pyributicarb |
| 别名 |
TSH-888 |
| 分子式 |
C18H22N2O2S |
| 分子量 |
330.44 |
| 溶解性 |
Soluble in DMSO |
| 纯度 |
≥98% |
| 外观(性状) |
White to off-white Solid |
| 储存条件 |
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| 运输条件 |
冷藏运输 |
| SMILES |
S=C(OC1=CC=CC(C(C)(C)C)=C1)N(C2=NC(OC)=CC=C2)C |
| InChIKey |
VTRWMTJQBQJKQH-UHFFFAOYSA-N |
| InChI |
InChI=1S/C18H22N2O2S/c1-18(2,3)13-8-6-9-14(12-13)22-17(23)20(4)15-10-7-11-16(19-15)21-5/h6-12H,1-5H3 |
| PubChem CID |
93486 |
| 靶点 |
Others |
| 通路 |
Others |
| 背景说明 |
Pyributicarb 是一种氨基甲酸酯型除草剂。 |
| 生物活性 |
Pyributicarb， a carbamate-type herbicide， is a potent activator of both CYP3A4 gene and human pregnane X receptor (hPXR).[1-2] |
| In Vitro |
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]. |
| In Vivo |
Pyributicarb causes enhancement of CYP3A4-derived reporter activity in mouse livers introduced with hPXR by adenovirus[1]. |
| 细胞实验 |
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]. |
| 动物实验 |
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]. |
| 数据来源文献 |
[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. |
| 规格 |
2mg 5mg 10mg 25mg 50mg 100mg |
| 单位 |
瓶 |
中文
英语
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