Zidovudine-Azidothymidine-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEZidovudineCat. No.: HY-17413CAS No.: 30516-87-1Synonyms: Azidothymidine; AZT; ZDV分式: CHNO分量: 267.24作靶點(diǎn): HIV; CRISPR/Cas9作通路: Anti-infection; Cell Cycle/DNA Damage儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 m

2、onth溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 100 mg/mL (374.20 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 3.7420 mL 18.7098 mL 37.4195 mL5 mM 0.7484 mL 3.7420 mL 7.4839 mL10 mM 0.3742 mL 1.8710 mL 3.7420 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVITY物活性

3、Zidovudine種核苷逆轉(zhuǎn)錄酶抑制劑 (NRTI)，泛于治療 HIV感染。Zidovudine 增強(qiáng) CRISPR/Cas9調(diào)節(jié)的編輯頻率。IC50 & Target HIV-1 CRISPR/Cas91/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE體外研究 Zidovudine inhibits SVG, Primary human fetal astrocytes (PFA), peripheral blood mononuclear cells (PBMC),and monocyte-derived macrophages (MDM)

4、 with EC50 of 17, 1311, 8, and 5 nM, respectively. Zidovudineinhibits SVG, PFA, PBMC, and MDM with EC90 of 0.205 M, 44.157 M, 0.481 M, and 0.219 M,respectively 1. Genome editing via CRISPR/Cas9 has become an efficient and reliable way to makeprecise, targeted changes to the genome of living cells. C

5、XCR4 is a co-receptor for the humanimmunodeficiency virus type 1 (HIV-1) infection and has been considered as an important therapeutic targetfor AIDS. CXCR4 mediates viral entry into human CD4+ cells by binding to envelope protein, gp120. HumanCXCR4 gene is efficiently disrupted by CRISPR/Cas9-media

6、ted genome editing, leading to HIV-1 resistanceof human primary CD4+ T cells. The Cas9-mediated ablation of CXCR4 demonstrated high specificity andnegligible off-target effects without affecting cell division and propagation 2.體內(nèi)研究 Intravitrous injection of the NRTIs Lamivudine (3TC), Zidovudine (AZ

7、T), or Abacavir (ABC) suppresses thelaser-induced choroidal neovascularization (CNV) in wild-type mice compared to PBS vehicle. The meanlevel of VEGF-A in the RPE/choroid, which peaks on day 3 after laser injury, is significantly reduced in 3TC-,AZT- and ABC-treated eyes compared with control eyes i

8、n wild-type mice, but not inP2rx7-/- mice 3.PROTOCOLCell Assay 1 Assays are performed in all cell types in the presence of titrating concentrations of ARV. 5,000 SVG, 2,500PFA, 200,000 PBMC, or 50,000 MDM cells/well are seeded into triplicate wells of 96-well plates. Twenty-fourhours later, the cult

9、ure medium is removed and replaced with medium containing the ARV or DMSO (0.5%vol/vol), and equivalent TCID50 infectious units of luciferase reporter virus are added to the cells. After a 16 hincubation at 37C, the initial viral inoculum is removed and replaced with culture medium containing thesam

10、e antiretroviral drug (ARV) or DMSO (0.5% vol/vol) concentrations. At 72 h post infection, the medium isaspirated, the cells are lysed and HIV-1 infection measured using the Luciferase Assay System.Luminescence is measured using a FLUOStar Optima microplate reader. Inhibition curves and the 50%(EC50

11、) and 90% (EC90) effective concentrations are determined by nonlinear regression analysis, usingGraphPad Prism software 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice 3Administration 3 C57BL/6J (wild-type) and P2rx7-/- mice are used. The

12、Nlrp3-/- mice are used. The NRTIs 3TC, AZT, andABC or the P2X7 antagonist A438079 hydrochloride are dissolved in PBS. For CNV, each group of mice isinjected once with 1 L of NRTIs (3TC, 125 ng/L; ABC, 183 ng/L; AZT, 146 ng/L), 1 L of A438079hydrochloride (3, 30, or 300 ng/L), or the same volume of v

13、ehicle (PBS) into the vitreous humor using a 33-gauge needle immediately after laser injury. Another group of mice is injected with 3TC (125 ng) incombination with an anti-mouse VEGF polyclonal antibody (10 ng). Goat whole IgG (10 ng) is used as abiological control for the anti-mouse VEGF antibody.M

14、CE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE1. Gray LR, et al. The NRTIs lamivudine, stavudine and zidovudine have reduced HIV-1 inhibitory activity in astrocytes. PLoS One. 2013Apr 16;8(4):e62196.2. Hou P, et al. Genome editing of CXCR4 by CRISPR/cas9 confers cells resistant to HIV-1 infection. Sci Rep. 2015 Oct 20;5:15577.3. Mizutani T, et al. Nucleoside Reverse Transcriptase Inhibitors Suppress Laser-Induced Choroidal Neovascularization in Mice. InvestOphthalmol Vis Sci.