1. Anti-infection
  2. HIV Reverse Transcriptase Parasite
  3. Nevirapine

Nevirapine  (Synonyms: 奈韦拉平; BI-RG 587; NSC 641530; NVP)

目录号: HY-10570 纯度: 99.93%
COA 产品使用指南

Nevirapine (BI-RG 587) 是用于研究 HIV/AIDS 的 HIV-1 逆转录酶非核苷抑制剂,Ki 值为 270 μM。

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Nevirapine Chemical Structure

Nevirapine Chemical Structure

CAS No. : 129618-40-2

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3.  试用装只面向终端客户

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥572
In-stock
5 mg ¥325
In-stock
10 mg ¥491
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50 mg ¥1100
In-stock
100 mg ¥1600
In-stock
200 mg ¥2600
In-stock
500 mg   询价  
1 g   询价  

* Please select Quantity before adding items.

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Top Publications Citing Use of Products
  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Nevirapine is a non-nucleoside inhibitor of HIV-1 reverse transcriptase used to treat and prevent HIV/AIDS; with a Ki of 270 μM[1].

IC50 & Target

HIV-1

 

体外研究
(In Vitro)

Nevirapine itself is an inhibitor of only CYP3A4 at concentrations that are well above those of therapeutic relevance (Ki=270 μM)[1]. Nevirapine has been used as a re-differentiation agent to treat cancers in several human cancer models. At all doses (100, 200, 350, 500 μM) tested, nevirapine significantly inhibits cell proliferation after 48 h treatment. At high dose (500 μM), nevirapine significantly increases the percentage of apoptotic cells compared with control[2]. Nevirapine is a potent and selective inhibitor (IC50=10-100 nM) of the replication of a wide variety of HIV-1 strains in several cellular assays[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Nevirapine is available for use in combination with nucleoside HIV-1 reverse transcriptase inhibitors (e.g., zidovudine, didanosine, etc.). Nevirapine 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 glucuronide conjugates of 2-, 3-, 8-, and 12-hydroxynevirapine[1]. Nevirapine is completely absorbed in both sexes of mouse, rat, rabbit, monkey, and chimpanzee. Nevirapine is extensively metabolized in both sexes of all animal species studied[4]. Nevirapine (9 mg/kg, 18 mg/kg and 36 mg/kg) shows significant reduction in ulcer severity score and ulcer index as compared to the control[5]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
分子量

266.30

Formula

C15H14N4O

CAS 号
性状

固体

颜色

White to off-white

中文名称

奈韦拉平;萘维拉平;那韦拉平;奈韦那平;萘韦拉平

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 14.29 mg/mL (53.66 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.7552 mL 18.7758 mL 37.5516 mL
5 mM 0.7510 mL 3.7552 mL 7.5103 mL
查看完整储备液配制表

* 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;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

In Vivo:

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 1.43 mg/mL (5.37 mM); 澄清溶液

    此方案可获得 ≥ 1.43 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 14.3 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% Corn Oil

    Solubility: ≥ 1.43 mg/mL (5.37 mM); 澄清溶液

    此方案可获得 ≥ 1.43 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。

    1 mL 工作液为例,取 100 μL 14.3 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料
参考文献
Cell Assay
[2]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[4]

Rats: 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, 26 μCi) for oral dosing to rats and 6.7 mg/mL (20.3 mg/kg, 10 μCi males, 8.9 μCi females) for intraduodenal administration to rats before bile collection. The i.v. dose is administered to rats (1.1 mg/kg, 20 μCi) as a solution in 20% ethanol/80% saline[4].

Mice: 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 μCi) with a specific activity of 5.55 μCi/mg for oral dosing to mice[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

完整储备液配制表

* 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;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.7552 mL 18.7758 mL 37.5516 mL 93.8791 mL
5 mM 0.7510 mL 3.7552 mL 7.5103 mL 18.7758 mL
10 mM 0.3755 mL 1.8776 mL 3.7552 mL 9.3879 mL
15 mM 0.2503 mL 1.2517 mL 2.5034 mL 6.2586 mL
20 mM 0.1878 mL 0.9388 mL 1.8776 mL 4.6940 mL
25 mM 0.1502 mL 0.7510 mL 1.5021 mL 3.7552 mL
30 mM 0.1252 mL 0.6259 mL 1.2517 mL 3.1293 mL
40 mM 0.0939 mL 0.4694 mL 0.9388 mL 2.3470 mL
50 mM 0.0751 mL 0.3755 mL 0.7510 mL 1.8776 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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HY-10570
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