Efavirenz是一种非核苷逆转录酶抑制剂（NNRTI）。
Cas No.:154598-52-4
Sample solution is provided at 25 µL, 10mM.
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Efavirenz is a non-nucleoside reverse transcriptase inhibitor (NNRTI). Efavirenz non-competitively inhibits the transcriptional (Ki=2.93nM) and replication (IC95=2.93nM) activity of HIV-1, thereby blocking viral replication. Efavirenz can be used in antiviral and anticancer research[1-4].
In vitro, Efavirenz (23.32–27.89μM) was used to treat triple-negative breast cancer cell lines MCF10AT, MCF10CA1α, and MDA-MB-231 for 4 days. Efavirenz significantly inhibited cell proliferation, reduced cell division, promoted apoptosis and necrosis, and induced a shift in cell morphology toward an epithelial-like phenotype[5]. Efavirenz (1.5μM) in combination with metformin (5 mM) and fluoxetine (0.9μM) was used to treat HCT116 human colon cancer cells for 24–96 hours. Efavirenz significantly increased cellular ROS levels, leading to cell death, decreased mitochondrial membrane potential and mitochondrial electron transport chain complex I and III activities, while increasing the expression of factors related to DNA damage, apoptosis, autophagy, and necroptosis[6].
In vivo, Efavirenz (10mg/kg) was orally administered to CD1 male mice for 36 days. Efavirenz significantly caused body weight loss and induced depression-like and anxiety-like behaviors[7]. Efavirenz (10mg/kg) was orally administered to CD1 male mice for 36 days. Efavirenz significantly led to body weight loss and increased the expression of appetite-related hormones[8].
References:
[1] Costa B, Vale N. Efavirenz: History, Development and Future. Biomolecules. 2022 Dec 31;13(1):88.
[2] Wang PF, Neiner A, Kharasch ED. Efavirenz Metabolism: Influence of Polymorphic CYP2B6 Variants and Stereochemistry. Drug Metab Dispos. 2019 Oct;47(10):1195-1205.
[3] Zhao T, Zhong R, Zhang X, et al. Efavirenz restored NMDA receptor dysfunction and inhibited epileptic seizures in GluN2A/Grin2a mutant mice. Front Neurosci. 2023 Mar 2;17:1086462.
[4] Ali T, Cashion J, Hannaoui S, et al. Treatment with efavirenz extends survival in a Creutzfeldt-Jakob disease model by regulating brain cholesterol metabolism. JCI Insight. 2025 Jun 19;10(14):e190296.
[5] Chiou PT, Ohms S, Board PG, et al. Efavirenz as a potential drug for the treatment of triple-negative breast cancers. Clin Transl Oncol. 2021 Feb;23(2):353-363.
[6] Kang BG, Shende M, Inci G, et al. Combination of metformin/efavirenz/fluoxetine exhibits profound anticancer activity via a cancer cell-specific ROS amplification. Cancer Biol Ther. 2023 Dec 31;24(1):20-32.
[7] Rojas-Osornio SA, Crespo-Ramírez M, Paredes-Cervantes V, et al. Oral Administration of Efavirenz Dysregulates the Tph2 Gene in Brain Serotonergic Areas and Alters Weight and Mood in Mice. Pharmaceuticals (Basel). 2024 Jun 18;17(6):801.
[8] Rojas-Osornio SA, Manuel-Apolinar L, Crespo-Ramírez M, et al. Efavirenz Interacts with Hormones Involved in Appetite and Satiety, Affecting Body Weight in Mice. Int J Mol Sci. 2026 Jan 11;27(2):735.
Efavirenz是一种非核苷逆转录酶抑制剂（NNRTI）。Efavirenz可非竞争性地抑制HIV-1的逆转（Ki=2.93nM）和复制（IC95=2.93nM）活性，从而阻断病毒复制。Efavirenz可用于抗病毒、抗癌症的相关研究[1-4]。
在体外，Efavirenz（23.32–27.89μM）处理三阴性乳腺癌细胞系MCF10AT、MCF10CA1α和MDA-MB-231 4天。Efavirenz显著抑制细胞增殖，减少细胞分裂，促进细胞凋亡和坏死，同时诱导细胞形态向上皮样表型分化[5]。Efavirenz（1.5μM）与metformin（5mM）和fluoxetine（0.9μM）组合处理HCT116人结肠癌细胞24-96小时。Efavirenz显著增加细胞ROS水平，导致细胞死亡，降低线粒体膜电位和线粒体电子传递链复合物I和III活性，同时增加DNA损伤、凋亡、自噬和坏死性凋亡相关因子的表达[6]。
在体内，Efavirenz（10mg/kg）口服给药于CD1雄性小鼠，持续36天。Efavirenz显著导致体重减轻并诱发抑郁样和焦虑样行为[7]。Efavirenz（10mg/kg）口服于CD1雄性小鼠，持续36天。Efavirenz显著导致体重减轻并增加食欲相关激素表达[8]。
| Cell experiment [1]: | |
Cell lines | MCF10AT, MCF10CA1α, MDA-MB-231 (triple-negative breast cancer cell lines) and MCF10A (non-cancerous breast epithelial cell line) |
Preparation Method | MCF10A, MCF10AT and MCF10CA1α cells were cultured in DMEM/F-12 medium supplemented with 5% horse serum, 10μg/ml insulin, 20ng/ml epidermal growth factor, 0.5μg/ml hydrocortisone, and 100ng/ml cholera toxin. MDA-MB-231 cells were cultured in DMEM medium with 10% fetal bovine serum. All cells were maintained at 37°C with 5% CO₂. Cells were treated with Efavirenz (23.32–27.89μM). |
Reaction Conditions | 23.32–27.89μM; 4 days |
Applications | Efavirenz caused cell death, retarded cell proliferation, and changed cell morphology to an epithelial-like phenotype in TNBC cell lines. Efavirenz also inhibited LINE-1 reverse transcriptase activity and downregulated fatty acid metabolism-associated genes (including SCD, ACSL5, FASN, ACSL3, FADS1, PTPLB and ACACA). |
| Animal experiment [2]: | |
Animal models | CD1 male mice |
Preparation Method | Mice were orally administered Efavirenz (10mg/kg) or distilled water (control) once daily for 36 days. At the end of treatment, behavioral tests were conducted, and brain tissues were collected for analysis. |
Dosage form | 10mg/kg; oral; once daily for 36 days |
Applications | Efavirenz administration resulted in significant body weight loss and increased food intake. Efavirenz induced depression-like behavior and anxiety-like behavior. Efavirenz also dysregulated Tph2 gene expression in the brainstem, hypothalamus, and amygdala, and increased 5-HT levels in the amygdala. |
References: | |
| Cas No. | 154598-52-4 | SDF | |
| 别名 | 依法韦仑; DMP 266; EFV; L-743726 | ||
| 化学名 | (4S)-6-chloro-4-(2-cyclopropylethynyl)-4-(trifluoromethyl)-1H-3,1-benzoxazin-2-one | ||
| Canonical SMILES | C1CC1C#CC2(C3=C(C=CC(=C3)Cl)NC(=O)O2)C(F)(F)F | ||
| 分子式 | C14H9ClF3NO2 | 分子量 | 315.68 |
| 溶解度 | ≥ 15.55mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.1678 mL | 15.8388 mL | 31.6776 mL |
| 5 mM | 633.6 μL | 3.1678 mL | 6.3355 mL |
| 10 mM | 316.8 μL | 1.5839 mL | 3.1678 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
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计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
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