Emtricitabine
(Synonyms: 恩曲他滨; BW1592) 目录号 : GC13653
A nucleoside reverse transcriptase inhibitor
Cas No.:143491-57-0
Sample solution is provided at 25 µL, 10mM.
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Emtricitabine is a nucleoside reverse transcriptase inhibitor (NRTI) with an EC50 of 0.01 µM in PBMC cell. It is an antiviral drug for the treatment of HIV infection.
Emtricitabine has in vitro activity against both laboratory strains of HIV-1 and HIV-2 and clinical isolates of HIV-1. The 50% effective concentration (EC50) ranges from 0.002 to 1.5 µ mol/L, depending on the viral isolate and cell line used. Emtricitabine demonstrates in vitro synergy with zidovudine and stavudine and additive in vitro activity when combines with zalcitabine or didanosine[1].
Reproductive and developmental toxicology studies are conducted with emtricitabine. Oral doses up to 1000 mg/kg/day provided daily area under the curve (AUC0→24) exposure to pregnant animals approximately 60- (mice) to 120-fold (rabbits) higher than that in humans at the recommended dose of 200 mg given once per day. In a mouse fertility study, emtricitabine had no effect on fertility, sperm count, or early embryonic development. There is no increased incidence of malformations in mouse and rabbit embryofetal toxicology studies. The development and fertility of F1 progeny are unaffected by emtricitabine in a mouse pre- and post-natal study. These data demonstrate a favorable pre-clinical reproductive safety profile for emtricitabine[2].
Reference：
[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]
Cell experiment: | 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]. |
Animal experiment: | 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]. |
References: [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. | |
| Cas No. | 143491-57-0 | SDF | |
| 别名 | 恩曲他滨; BW1592 | ||
| 化学名 | 4-amino-5-fluoro-1-[(2R,5S)-2-(hydroxymethyl)-1,3-oxathiolan-5-yl]pyrimidin-2-one | ||
| Canonical SMILES | C1C(OC(S1)CO)N2C=C(C(=NC2=O)N)F | ||
| 分子式 | C8H10FN3O3S | 分子量 | 247.25 |
| 溶解度 | ≥ 10.4mg/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 | 4.0445 mL | 20.2224 mL | 40.4449 mL |
| 5 mM | 0.8089 mL | 4.0445 mL | 8.089 mL |
| 10 mM | 0.4044 mL | 2.0222 mL | 4.0445 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 | ||||||||||
| 计算重置 | ||||||||||
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.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet