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- 技术资料
- 保存条件：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
Emtricitabine
- 库存：
999
- 供应商：
北京索莱宝科技有限公司
- CAS号：
143491-57-0
- 规格：
50mg/25mg/100mg/500mg
| 规格： | 50mg | 产品价格： | ¥490.00 |
|---|---|---|---|
| 规格： | 25mg | 产品价格： | ¥364.00 |
| 规格： | 100mg | 产品价格： | ¥790.00 |
| 规格： | 500mg | 产品价格： | ¥1340.00 |
| CAS | 143491-57-0 |
| 中文名称 | 恩曲他滨 |
| 英文名称 | Emtricitabine |
| 别名 | 恩曲他滨; BW1592 |
| 分子式 | C8H10FN3O3S |
| 分子量 | 247.25 |
| 规格 | 50mg ; 25mg ; 100mg ; 500mg |
| 溶解性 | Soluble in Water/DMSO ≥3mg/mL |
| 纯度 | ≥98% |
| 级别 | Cell Culture |
| 外观(性状) | White to off-white Solid |
| 储存条件 | Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| 运输条件 | 冷藏运输 |
| EC | EINECS 604-363-1 |
| MDL | MFCD00870151 |
| SMILES | C1[C@H](O[C@H](S1)CO)N2C=C(C(=NC2=O)N)F |
| InChIKey | XQSPYNMVSIKCOC-NTSWFWBYSA-N |
| InChI | InChI=1S/C8H10FN3O3S/c9-4-1-12(8(14)11-7(4)10)5-3-16-6(2-13)15-5/h1，5-6，13H，2-3H2，(H2，10，11，14)/t5-，6+/m0/s1 |
| PubChem CID | 60877 |
| 靶点 | HIV;HBV |
| 通路 | Anti-infection |
| 背景说明 | Emtricitabine对人类免疫缺陷病毒HIV和HBV具有抑制活性。 |
| 生物活性 | Emtricitabine is a nucleoside reverse transcriptase inhibitor (NRTI) with an EC50 of 0.01 μM in PBMC cell. It is an antiviral agent for the treatment of HIV infection.[1-4] |
| In Vitro | Emtricitabine 对 HIV-1 和 HIV-2 的实验室菌株以及 HIV-1 的临床分离株均具有体外活性。50% 有效浓度 (EC50) 范围为 0.002 至 1.5 μmol/L，具体取决于所使用的病毒分离物和细胞系。Emtricitabine 与齐多夫定和司他夫定体外协同作用，当与扎西他滨或去羟肌苷联合使用时体外活性[1]。 |
| In Vivo | 生殖和发育毒理学研究是用 Emtricitabine 进行的。口服剂量高达每天一次 1000 mg/kg/day 时，暴露于妊娠动物的每日曲线下面积 (AUC0→24) 约为 60-(小鼠) 至 120 倍 (兔) ，高于人类的推荐剂量 （200 毫克）。在一项小鼠生育力研究中，Emtricitabine 对生育力、精子数量或早期胚胎发育没有影响。在小鼠和兔胚胎胎儿毒理学研究中没有增加畸形发生率。在小鼠产前和产后研究中，F1 后代的发育和生育能力不受 Emtricitabine 的影响。这些数据表明 Emtricitabine 具有良好的临床前生殖安全性[2]。 |
| 细胞实验 | EA.hy926 cells were plated in a 12-， 24- or 96-well plates and grown in DMEM media supplemented with 3% FCS. Endothelial cells from PARP+/+and PARP-/- mice were isolated and cultured. Cell viability was determined by the reduction of yellow MTT into a purple formazan product by mitochondrial dehydrogenases of metabolically active cells. Following the treatment period， the experimental medium was removed and 100 μL MTT (1 mg/mL) added. After 1 h incubation， the MTT solution was carefully removed and the purple crystals were solubilized in 100 μL of DMSO. The DMSO was transferred to an ELISA plate and absorbance measured at 550 nm with a 620 nm[3]. |
| 动物实验 | Mice: Emtricitabine (free base) is suspended in 0.5% aqueous methylcellulose and given by gavage， with the daily dose divided into two equal installments administered approximately 6 h apart. The dose volume is 5 mL/kg/dose (10 mL/kg/day). In 1- and 6-month oral toxicity studies in mice， the maximum tolerated dose of emtricitabine is >3000 mg/kg/day. However， dose-range-finding studies are performed in pregnant CD-1 mice and in New Zealand White rabbits at top doses of 1000 mg/kg/day[2]. Rabbits: Mature artificially inseminated rabbits are given emtricitabine on gestational day 7 through 19. On gestational day 19， blood samples for toxicokinetics are taken from five satellite does in each group at 30–60 min prior to dosing， and at 1， 3， 7， and 12 h after the first daily-dose (prior to the second daily-dose). On gestational day 20， the satellite does are sacrificed at 1 h after the final dose， and maternal blood and fetal umbilical blood samples are collected for toxicokinetics[2]. |
| 数据来源文献 | [1]. Saag MS， et al. Emtricitabine， a new antiretroviral agent with activity against HIV and hepatitis B virus. Clin Infect Dis.?2006 Jan 1;42(1):126-31. [2]. Xu P， et al. Combined Medication of Antiretroviral Drugs Tenofovir Disoproxil Fumarate， Emtricitabine， and Raltegravir Reduces Neural Progenitor Cell Proliferation In Vivo and In Vitro. J Neuroimmune Pharmacol. 2017 Dec;12(4):682-692. [3]. Szczech GM， Wang LH， Walsh JP， Reproductive toxicology profile of emtricitabine in mice and rabbits. Reprod Toxicol. 2003 Jan-Feb;17(1):95-108. [4]. Faltz M， et al. Effect of the Anti-retroviral Drugs Efavirenz， Tenofovir and Emtricitabine on Endothelial Cell Function: Role of PARP. Cardiovasc Toxicol. 2017 Jan 3. [Epub ahead of print] |
| 单位 | 瓶 |
| 表格1 | |*|1mg|5mg|10mg|$$|1mM|4.0445mL|20.2224mL|40.4449mL|$$|5mM|0.8089mL|4.0445mL|8.089mL|$$|10mM|0.4044mL|2.0222mL|4.0445mL| |
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恩曲他滨
¥364 - 1340
