Nevirapine

CAS号

129618-40-2

分子式

C15H14N4O

主要靶点

Reverse Transcriptase|HIV Protease

仅限科研使用

Cat No : CM01066

Print datasheet

Synonyms

inhibit|Human immunodeficiency virus|HIV Protease|HIVProtease|HIV-1 reverse transcriptase|HIV|BI-RG 587|BI-RG587|BI-RG-587|奈韦拉平|奈伟拉平|Reverse Transcriptase|ReverseTranscriptase|NVP|NSC641530|NSC-641530|Nevirapine|NSC 641530|Inhibitor



产品信息

CAS号 129618-40-2
分子式 C15H14N4O
主要靶点 Reverse Transcriptase|HIV Protease
主要通路 微生物学|微生物学|蛋白酶体
分子量 266.3
纯度 99.6%, 此纯度可做参考,具体纯度与批次有关系,可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 inhibit|Human immunodeficiency virus|HIV Protease|HIVProtease|HIV-1 reverse transcriptase|HIV|BI-RG 587|BI-RG587|BI-RG-587|奈韦拉平|奈伟拉平|Reverse Transcriptase|ReverseTranscriptase|NVP|NSC641530|NSC-641530|Nevirapine|NSC 641530|Inhibitor

靶点活性

HIV-1:270 μM(ki)

体内活性

Nevirapine(NVP)本身仅为CYP3A4的抑制剂,且抑制浓度远高于治疗相关(Ki:270 μM)的浓度。 作为非核苷逆转录酶抑制剂,Nevirapine可有效抑制逆转录病毒来源的逆转录酶。Nevirapine也可有效抑制鼠和人细胞系中的内源性逆转录。Nevirapine可挽救急性髓系白血病(AML)细胞系和AML患者的原发细胞中存在的分化阻滞,如形态学、功能和免疫表型分析所示。 Nevirapine使RNA酶H的切割特异性发生改变,导致Nevirapine诱发的核糖核酸酶H活性超过切割特异性变化的预期。Nevirapine是HIV-1逆转录酶(RT)的高特异性抑制剂,在酶分析中IC50为84 nM,在细胞培养物中抗HIV-1复制的IC50为40 nM。

体外活性

Nevirapine(NVP)各类动物体内的代谢情况如下:除雄性大鼠以外所有动物的粪便主要代谢物之一是3- OHNVP.所有雄性动物和雌性小鼠,狗和猴的主要代谢物之一是4- CANVP.大鼠胆汁的主要代谢物是4- CANVP和12-OHNVP葡糖苷酸.

溶解度

DMSO:18.33 mg/mL (68.84 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble)

细胞实验

FRO cells are seeded into 96-well culture plates at 10,000 cells/well. Cells are treated with different doses of nevirapine (0, 100, 200, 350 and 500 μM) for 48 h. MTT dye (5 mg/mL) is added to each well for additional 4 h, and the reaction is then stopped by the addition of DMSO. Optical density is measured at 490 nm on a multi-well plate reader[2].

参考文献

1.Erickson DA, et al. Drug Metab Dispos, 1999, 27(12), 1488-1495.
2.Zhang R, Zhang F, Sun Z, et al. LINE-1 Retrotransposition Promotes the Development and Progression of Lung Squamous Cell Carcinoma by Disrupting the Tumor Suppressor Gene FGGY[J]. Cancer research. 2019: canres. 0076.2019.
3.Mangiacasale R, et al. Oncogene, 2003, 22(18), 2750-2761.
4.Grob PM, et al. AIDS Res Hum Retroviruses, 1992, 8(2), 145-152.
5.Palaniappan C, et al. J Biol Chem, 1995, 270(9), 4861-4869.
6.Riska PS, et al. Drug Metab Dispos, 1999, 27(12), 1434-1447.
7.Onasanwo SA, et al. Evaluation of anti-ulcerogenic and ulcer-healing activities of nevirapine in rats. Afr J Med Med Sci. 2015 Sep;44(3):251-9.
8.Wu Y, Yang J, Duan C, et al. Simultaneous determination of antiretroviral drugs in human hair with liquid chromatography-electrospray ionization-tandem mass spectrometry[J]. Journal of Chromatography B. 2018 Apr 15;1083:209-221.
9.Tan S, Li W, Li Z, et al. A Novel CXCR4 Targeting Protein SDF-1/54 as an HIV-1 Entry Inhibitor. Viruses. 2019, 11(9): 874.
10.Tan S, Li J Q, Cheng H, et al. The anti-parasitic drug suramin potently inhibits formation of seminal amyloid fibrils and their interaction with HIV-1[J]. Journal of Biological Chemistry. 2019: jbc. RA118. 006797.

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
=
×
×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
×
=
×
C1   V1   C2   V2