奈韦拉平作用机制 - Medchemexpress - MCE中国

1、Product Data SheetNevirapineCat. No.: HY-10570CAS No.: 129618-40-2分式: CHNO分量: 266.3作靶点: HIV; Reverse Transcriptase作通路: Anti-infection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 : 14.29 mg/mL (53.66 mM; Need ultrasonic)SolventMass1 mg 5 mg 10 mgConcentration制备

2、储备液1 mM 3.7552 mL 18.7758 mL 37.5516 mL5 mM 0.7510 mL 3.7552 mL 7.5103 mL10 mM 0.3755 mL 1.8776 mL 3.7552 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；旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 储存时，请在 6 个内使，-20C 储存时，请在 1 个内使。体内实验请根据您的实验动物和给药式选择适当的溶解案。以下溶解案都请先按照 In Vitro 式配制澄清的储备液，再依次添加

3、助溶剂：为保证实验结果的可靠性，澄 的储备液可以根据储存条件，适当保存；体内实验的作液，建议您现现配，当天使； 以下溶剂前显的百分 指该溶剂在您配制终溶液中的体积占；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的式助溶1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 1.43 mg/mL (5.37 mM); Clear solution此案可获得 1.43 mg/mL (5.37 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 14.299999 mg/mL 的澄清DMS

4、O 储备液加到 400 L PEG300 中，混合均匀；向上述体系中加 50 L Tween-80，混合均匀；然后继续加 450 L 理盐定容 1 mL。2. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 1.43 mg/mL (5.37 mM); Clear solution此案可获得 1.43 mg/mL (5.37 mM，饱和度未知) 的澄 溶液，此案不适于实验周 期在半个以上的实验。Page 1 of 2 www.MedChemE以 1 mL 作液为例，取 100 L 14.299999 mg/mL 的澄 DMSO 储备液加到 900 L 油中

5、，混合均匀。BIOLOGICAL ACTIVITY物活性 Nevirapine于治疗和预防HIV/AIDS的HIV-1逆转录酶核苷抑制剂，Ki值为270 M。IC & Target Ki: 270 M (HIV-1 reverse transcriptase)1体外研究 Nevirapine itself is an inhibitor of only CYP3A4 at concentrations that are well above those of therapeutic relevance (Ki=270 M)1. Nevirapine has been used as a re-

6、differentiation agent to treat cancers in several human cancer models.At all doses (100, 200, 350, 500 M) tested, nevirapine significantly inhibits cell proliferation after 48 h treatment. Athigh dose (500 M), nevirapine significantly increases the percentage of apoptotic cells compared with control

7、2.Nevirapine is a potent and selective inhibitor (IC50=10-100 nM) of the replication of a wide variety of HIV-1 strains inseveral cellular assays3.体内研究 Nevirapine is available for use in combination with nucleoside HIV-1 reverse transcriptase inhibitors (e.g., zidovudine,didanosine, etc.). Nevirapin

8、e has received FDA approval for use in combination with HIV-1 protease inhibitors (e.g.,saquinavir, ritonavir, indinavir, etc.). In humans, nevirapine is eliminated primarily in the urine as glucuronideconjugates of 2-, 3-, 8-, and 12-hydroxynevirapine1. Nevirapine is completely absorbed in both sex

9、es of mouse, rat,rabbit, monkey, and chimpanzee. Nevirapine is extensively metabolized in both sexes of all animal species studied4.Nevirapine (9 mg/kg, 18 mg/kg and 36 mg/kg) shows significant reduction in ulcer severity score and ulcer index ascompared to the control5PROTOCOLCell Assay 2 FRO cells

10、 are seeded into 96-well culture plates at 10,000 cells/well. Cells are treated with different doses ofnevirapine (0, 100, 200, 350 and 500 M) for 48 h. MTT dye (5 mg/mL) is added to each well for additional 4 h, andthe reaction is then stopped by the addition of DMSO. Optical density is measured at

11、 490 nm on a multi-well platereader2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Rats: Nevirapine and 14C Nevirapine are dissolved together in absolute ethanol and methylene chloride (1:1, v/v)Administration 4 with mild heating. The concentra

12、tion of drug in suspension is 2 mg/mL (20 mg/kg, 26 Ci) for oral dosing to rats and6.7 mg/mL (20.3 mg/kg, 10 Ci males, 8.9 Ci females) for intraduodenal administration to rats before bile collection.The i.v. dose is administered to rats (1.1 mg/kg, 20 Ci) as a solution in 20% ethanol/80% saline4.Mic

13、e: Nevirapine and 14C Nevirapine are dissolved together in absolute ethanol and methylene chloride (1:1, v/v)with mild heating. The concentration of drug in suspension is 2 mg/mL (20 mg/kg, 2.5 Ci) with a specific activity of5.55 Ci/mg for oral dosing to mice4.MCE has not independently confirmed the

14、 accuracy of these methods. They are for reference only.户使本产品发表的科研献 Int J Antimicrob Agents. 2019 Dec;54(6):814-819.Page 2 of 3 www.MedChemESee more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Erickson DA, et al. Characterization of the in vitro biotransformation of the H

15、IV-1 reverse transcriptase inhibitornevirapine by human hepaticcytochromes P-450. Drug Metab Dispos. 1999 Dec;27(12):1488-95.2. Dong JJ, et al. In vitro evaluation of the therapeutic potential of nevirapine in treatment of human thyroid anaplastic carcinoma. Mol Cell Endocrinol.2013 May 6;370(1-2):1

16、13-8.3. Merluzzi VJ, et al. Inhibition of HIV-1 replication by a nonnucleoside reverse transcriptase inhibitor. Science. 1990 Dec 7;250(4986):1411-3.4. Riska PS, et al. Biotransformation of nevirapine, a non-nucleoside HIV-1 reverse transcriptase inhibitor, in mice, rats, rabbits, dogs, monkeys, andchimpanzees. Drug Metab Dispos. 1999 Dec;27(12):1434-47.5. Onasanwo SA, et al. Evaluation of anti-ulcerogenic and ulcer-healing activities of nevirapine in rats. Afr J Med Me