1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEPyributicarbCat. No.: HY-111202CAS No.: 88678-67-5Synonyms: TSH-888分式: CHNOS分量: 330.44作靶點: Cytochrome P450作通路: Metabolic Enzyme/Protease儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 100 m

2、g/mL (302.63 mM; Need ultrasonic)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (7.57 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (7.57 mM); Suspended solution; Need ultrasonic1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemE3. 請依序添加每種溶劑： 1

3、0% DMSO 90% corn oilSolubility: 2.5 mg/mL (7.57 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Pyributicarb種氨 甲酸酯型除草劑， CYP3A4 因和類孕烷 X 受體 (hPXR) 的有效激活劑。IC50 & Target CYP3A4 1, hPXR 2體外研究 Pyributicarb, a carbamate-type herbicide, is a potent activator of both CYP3A4 gene and human pregnane Xreceptor (hPXR)

4、. Pyributicarb is found to increase the CYP3A4 reporter activity at 0.1 to 1 M more stronglythan 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 inHepG2

5、 cells 1. Pyributicarb induces luciferase transcription via hPXR at low concentrations in the order of10 nM. The relative potency of Pyributicarb for hPXR is 8.6-fold that of rifampicin (RIF) 2.體內研究 Pyributicarb causes enhancement of CYP3A4-derived reporter activity in mouse livers introduced with h

6、PXRby adenovirus 1.PROTOCOLCell Assay 1 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 M Pyributicarb for 48 h. Then reporter activities are determined 1.MCE has not independently confirmed the accuracy o

7、f these methods. They are for reference only.Animal Male ICR mice (5 weeks old) are used and fed standard rodent chow. After 18-h fasting, mice are injected i.v.Administration 1 with adenovirus 4.0 109 50% titer culture infectious dose (TCID50)/mouse. Three days after the infection,vehicle (0.5% met

8、hyl cellulose/saline) or Pyributicarb (100 mg/kg/day) is administered p.o. for 2 consecutivedays. Animals are killed 20 h after the last dose 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Matsubara T, et al. Assessment of human pregnane

9、 X receptor involvement in pesticide-mediated activation of CYP3A4 gene. DrugMetab 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 reportergene assays. Toxicology. 2011 Feb 27;280(3):77-87.McePdfHeightCaution: Product has not been fully validated for medic