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My CartCAS：129618-40-2
Molecular Formula：C15H14N4O
Molecular Weight：266.3
Storage：Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to off-white Solid
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| CAS | 129618-40-2 |
| Name | Nevirapine |
| Molecular Formula | C15H14N4O |
| Molecular Weight | 266.3 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC | EINECS 603-345-0 |
| MDL | MFCD00866928 |
| SMILES | O=C1C2=C(N=CC=C2)N(C3CC3)C4=NC=CC(C)=C4N1 |
| InChIKey | NQDJXKOVJZTUJA-UHFFFAOYSA-N |
| InChI | InChI=1S/C15H14N4O/c1-9-6-8-17-14-12(9)18-15(20)11-3-2-7-16-13(11)19(14)10-4-5-10/h2-3,6-8,10H,4-5H2,1H3,(H,18,20) |
| PubChem CID | 4463 |
| Target Point | HIV |
| Passage | Anti-infection |
| Background | Nevirapine is a non-nucleoside inhibitor of HIV-1 reverse transcriptase. |
| Biological Activity | Nevirapine是用于治疗和预防HIV/AIDS的HIV-1逆转录酶非核苷抑制剂，Ki值为270 μM。[1-5] |
| In Vitro | 奈韦拉平本身仅是CYP3A4的抑制剂，其浓度远高于治疗相关性(Ki =270μM)[1]。奈韦拉平已被用作再分化剂，用于治疗几种人类癌症模型中的癌症。在所有测试的剂量(100，200，350，500μM)下，奈韦拉平在48小时处理后显著抑制细胞增殖。在高剂量(500μM)下，与对照相比，奈韦拉平显著增加凋亡细胞的百分比[2]。在几种细胞试验中，奈韦拉平是一种有效的选择性抑制剂(IC50 = 10-100 nM)，可以复制多种HIV-1菌株[3]。 |
| In Vivo | 奈韦拉平可与核苷HIV-1逆转录酶抑制剂(例如，齐多夫定，去羟肌苷等)组合使用。奈韦拉平已获得FDA批准与HIV-1蛋白酶抑制剂(如沙奎那韦，利托那韦，茚地那韦等)联合使用。在人类中，奈韦拉平主要在尿液中作为2-，3-，8-和12-羟基奈韦拉平的葡糖苷酸结合物被消除[1]。奈韦拉平完全被小鼠，大鼠，兔子，猴子和黑猩猩的性别所吸收。奈韦拉平在研究的所有动物物种的两性中都有广泛代谢[4]。与对照组相比，奈韦拉平(9 mg/kg，18 mg/kg和36 mg/kg)显示溃疡严重程度评分和溃疡指数显著降低[5] |
| Cell Experiment | 将FRO细胞以10，000个细胞/孔接种到96孔培养板中。用不同剂量的奈韦拉平(0，100，200，350和500μM)处理细胞48小时。将MTT染料(5mg/mL)加入各孔中另外4小时，然后通过加入DMSO终止反应。在多孔板读数器上测量490nm处的光密度[2]。 |
| Animal Experiment | 大鼠：将奈韦拉平和[14 C]奈韦拉平在无水乙醇和二氯甲烷(1：1，v/v)中一起溶解，同时温和加热。对于大鼠口服给药，悬浮液中的药物浓度为2mg/mL(20mg/kg，26μCi)，对于大鼠十二指肠内给药，为6.7mg/mL(20.3mg/kg，10μCi雄性，8.9μCi雌性)。胆汁收集。静脉注射给大鼠(1.1mg/kg，20μCi)，为20％乙醇/ 80％盐水溶液[4]。小鼠：奈韦拉平和[14 C]奈韦拉平在无水乙醇和二氯甲烷(1：1，v/v)中一起溶解，同时温和加热。悬浮液中的药物浓度为2 mg/mL(20 mg/kg，2.5μCi)，对小鼠口服给药的比活性为5.55μCi/ mg [4]。 |
| Data Literature Source | [1]. Erickson DA，et al. Characterization of the in vitro biotransformation of the HIV-1 reverse transcriptase inhibitornevirapine by human hepatic cytochromes 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):113-8. [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，and chimpanzees. 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 Med Sci. 2015 Sep;44(3):251-9. |
| Unit | Piece |
| Specification | 10mg 20mg 50mg |
Nevirapine是HIV-1逆转录酶非核苷抑制剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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