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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEBenzoapyreneCat. No.: HY-107377CAS No.: 50-32-8Synonyms: 3,4-Benzopyrene分式: CH分量: 252.31作靶点: Others作通路: Others储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 50 mg/mL (198.17 mM; Need ultra
2、sonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 3.9634 mL 19.8169 mL 39.6338 mL5 mM 0.7927 mL 3.9634 mL 7.9268 mL10 mM 0.3963 mL 1.9817 mL 3.9634 mL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,并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Benzoapyrene 在动物模型中显肺致癌性,并且它们经常于化学预防研究。体内研究Statistically signifi
3、cant decrease is observed at 7 weeks in females receiving 1.0 mg Benzoapyrene (BaP)compare with the vehicle group. As lung tumorigenesis induced by Benzoapyrene is dose dependent infemale A/J mice. The incidence of hyperplasia values in females treating with 0.25, 0.50, and 1.0 mgBenzoapyrene are si
4、gnificantly higher than in the vehicle-treated group. The incidence of adenoma in1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEfemales receiving 1.0 mg Benzoapyrene is significantly higher than in the vehicle group. The multiplicity ofhyperplasia in females receiving 0.50 or 1.0 mg Benzoapyrene i
5、s significantly higher than in the vehiclegroup. The multiplicity of adenoma in the group treated with 1.0 mg is also significantly higher than in thevehicle group. The incidences of hyperplasia and adenoma in female A/J mice are significantly increased byBenzoapyrene in a dose-dependent manner 1. B
6、enzoapyrene induces an average of 9.381.75 tumorswith an average tumor load of 19.533.81 mm3 (P 2.PROTOCOLAnimal Female A/J mice are randomized into eight groups (n=8): (i) control; (ii)Benzoapyrene (B(a)P)+vehicleAdministration 2 (methocel); (iii) Benzoapyrene+roflumilast 1 mg/kg; (iv) Benzoapyrene
7、+roflumilast 5 mg/kg; (v)Benzoapyrene+aerozolie phosphate-buffer saline (PBS); (vi) Benzoapyrene+aerosolize budesonide 2.25mg/mL; (vii) Benzoapyrene+aerosolized budesonide 2.25 mg/mL+roflumilast 1 mg/kg; and (viii)Benzoapyrene+aerosolize budesonide 2.25 mg/mL+roflumilast 5 mg/kg groups. A single dos
8、e ofBenzoapyrene in corn oil is given intraperitoneally once at 100 mg/kg body weight. Roflumilast (1 or 5mg/kg) is started 2 weeks after Benzoapyrene. It is continued for 26 weeks (3 days/week) via oral gavage.Mice in the Benzoapyrene+vehicle group are treated with an equal volume of methocel as so
9、lvent control.Aerosolizing budesonide is administrated by inhaling route as an aerosol at a dose of 2.25 mg/mL for 2 minper application at 2 weeks after Benzoapyrene. It is continued for 26 weeks (5 days/week). PBS is alsoused as solvent control by inhaling route after Benzoapyrene administration in
10、 the Benzoapyrene+PBSgroup. Mice are killed at 28 weeks after exposure to Benzoapyrene. Their lungs are excised and stored at -70 C 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Saeko Onami, et al. Dosimetry for lung tumorigenesis induc
11、ed by urethane, 4-(N-methyl-N-nitrosamino)-1-(3-pyridyl)-1-butanone (NNK),and benzoapyrene (BaP) in A/JJmsSlc mice. J Toxicol Pathol. 2017 Jul; 30(3): 209216.2. Yeo CD, et al. Roflumilast treatment inhibits lung carcinogenesis in benzo(a)pyrene-induced murine lung cancer model. Eur JPharmacol. 2017 Oct 5;812:189-McePdfHeightCaution: Product has not
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