1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEPiperineCat. No.: HY-N0144CAS No.: 94-62-2Synonyms: Bioperine; 1-Piperoylpiperidine分式: CHNO分量: 285.34作靶點(diǎn): P-glycoprotein; Autophagy作通路: Membrane Transporter/Ion Channel; Autophagy儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C

2、 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 31 mg/mL (108.64 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 3.5046 mL 17.5230 mL 35.0459 mL5 mM 0.7009 mL 3.5046 mL 7.0092 mL10 mM 0.3505 mL 1.7523 mL 3.5046 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。BIOLOGI

3、CAL ACTIVITY物活性 Piperine從胡椒中分離的天然物堿，可以抑制P-glycoprotein and CYP3A4的活性，在HeLa細(xì)胞中的IC50值為61.940.054 g/mL。IC50 & Target IC50: 61.940.054 g/mL (P-glycoprotein, HeLa cell) 11/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE體外研究 Piperine has shown to possess in vitro cytotoxic activity and in silico studies.

4、The IC50 value is found to be61.940.054 g/mL and in silico studies, it has more number of hydrogen bonds with minimum binding anddocking energy and may be considered as inhibitor of EGFR tyrosine kinase 1. Piperine has been found tohave immunomodulatory, anti-oxidant, anti-asthmatic, anti-carcinogen

5、ic, anti-inflammatory, anti-ulcer, andanti-amoebic properties 2. Piperine could enhance the bioavailabilities of other drugs including rosuvastatin,peurarin and docetaxel (DOX) via inhibition of CYP3A and P-glycoprotein activity 3.體內(nèi)研究 At the dose of 3.5 mg/kg, the bioavailability of piperine is cal

6、culated to be 25.36%. Its AUC0t isunproportionally increased with doses, indicating a potential non-linear pharmacokinetics profile of piperine. Itis found that the AUC0t and C0 of docetaxel and t1/2of piperine are significantly increased after theircombination use, suggesting potential enhanced bio

7、availability of not only docetaxel but also piperine, whichmay lead to the overall enhanced pharmacological effects 3. The phosphorylation of I-B, p65, p38, ERK,and JNK is inhibited by piperine in a dose-dependent manner, indicating that piperine may be a potential anti-inflammatory drug both in end

8、ometritis and in other S. aureus-induced diseases 4.PROTOCOLCell Assay 1 Standard solution is prepared by dissolving 10 mg of piperine in 100 mL of methanol. The MTT assay iscarried out to measure cell viability. Ten thousand cells in 100 L of DMEM media are seeded in the wells ofa 96-well plate. Af

9、ter 24 h, existing media is removed and 100 L of various concentrations of piperine(20100 g/mL) are added and incubated for 48 h at 37 C in a CO2 incubator. Control cells aresupplemented with 0.05 % DMSO vehicle. At the 48th hour of incubation, MTT (10 L of 5 mg/mL) is addedto the plate. The content

10、s of the plate are pipetted out carefully, the formazan crystals formed are dissolvedin 100 L of DMSO, and the absorbance is measured at 550 nm in a microplate reader 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Rats: The stock solutions of

11、piperine (PIP) and docetaxel (DOX)are prepared by dissolving appropriateAdministration 34 amount of each authentic compound in DMSO separately at 1 mg/mL. The standard solutions containingboth PIP and DOX are prepared by serial dilution of the stock solutions with 0.2% formic acid and acetonitrile(5

12、0:50, v/v) to yield concentrations of 25, 50, 100, 200, 400, 800, 1600, 3200, 6400, 12800 ng/mL. 25Sprague-Dawley rats are divided into five groups receiving DOX(Group DOX 7 iv, 7 mg/kg, i.v.), PIP (GroupPIP 35 po, 35 mg/kg,p.o.) and their combined administration (Group DOX+PIP) as well as PIP (Grou

13、p PIP3.5 po, 3.5 mg/kg, p.o.) and PIP (Group PIP 3.5 iv, 3.5 mg/kg, i.v.) 3.Mice: Piperine is dissolved in 5 mL of tris buffered saline (TBS) at concentrations corresponding to 25, 50,and 100 mg/kg, based on the weight of the mice. After 24 h of S. aureus infection in the uterus, the piperinesolutio

14、n is injected intraperitoneally three times every 6 h. A total of 60 female BALB/c mice are used in thisstudy. All mice are maintained on a 12 h light/dark cycle and cafeteria feeding 4.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) PLoS Bi

15、ol. 2018 Jul 12;16(7):e2004921.2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE J Neurosci Res. 2019 Aug 16. Int Immunopharmacol. 2018 Oct 30;65:448-457. Biochem Biophys Res Commun. 2019 Aug 20;516(2):365-372.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Paarakh PM, et al. I

16、n vitro cytotoxic and in silico activity of piperine isolated from Piper nigrum fruits Linn. In Silico Pharmacol. 2015Dec;3(1):9. Epub 2015 Oct 29.2. Meghwal M,et al. Piper nigrum and piperine: an update. Phytother Res. 2013 Aug;27(8):1121-30.3. Li C, et al. Non-linear pharmacokinetics of piperine and its herb-drug interactions with docetaxel in Sprague-Dawley rats. J PharmBiomed Anal. 2016 Sep 5;128:286-93.4. Zhai WJ, et al. Piperine Plays an Anti-Inflammatory Role in Staphylococcus aureus Endometritis by Inhibiting Activation of NF-B andMAPK Pathways in Mice.