Dynasore _Dynamin 抑制劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEDynasoreCat. No.: HY-15304CAS No.: 304448-55-3分式: CHNO分量: 322.31作靶點(diǎn): Dynamin; Autophagy作通路: Cytoskeleton; Autophagy儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 50 mg/mL (155.13 mM)* mean

2、s soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 3.1026 mL 15.5130 mL 31.0260 mL5 mM 0.6205 mL 3.1026 mL 6.2052 mL10 mM 0.3103 mL 1.5513 mL 3.1026 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。體內(nèi)實(shí)驗(yàn) 請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前?qǐng)先配制澄清的儲(chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建

3、議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (7.76 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (7.76 mM); Clear solution1/3 Master of Small Molecules 您邊的抑制劑師www.Med

4、ChemEBIOLOGICAL ACTIVITY物活性 Dynasore可滲透細(xì)胞的發(fā)動(dòng)蛋抑制劑，IC50為15 M。IC50 & Target IC50: 15 M (GTPase activity of dynamin1 and 2) 1體外研究 Dynasore interferes with the GTPase activity of dynamin1, dynamin2, and Drp1, the mitochondrial dynamin,but not of other small GTPases. Dynasore acts as a potent inhibitor of

5、 endocytic pathways known to dependon dynamin by rapidly blocking coated vesicle formation within seconds of dynasore addition. Two types ofcoated pit intermediates accumulate during dynasore treatment, g-shaped, half formed pits and O-shaped,fully formed pits, captured while pinching off 1. Dynasor

6、e inhibits HSV-1 and HSV-2 infection of humanepithelial and neuronal cells, including primary genital tract cells and human fetal neurons and astrocytes.Dynasore reduces the number of viral capsids reaching the nuclear pore if added at the time of viral entryand that, when added as late as 8 h poste

7、ntry, dynasore blocks the transport of newly synthesized viralproteins from the nucleus to the cytosol 2. Dynasore prevents ischemia/reperfusion induced elevation of leftventricular end diastolic pressure. Dynasore also decreases cardiac troponin I efflux during reperfusion andreduces infarct size.

8、In cultured adult mouse cardiomyocytes subjected to oxidative stress, dynasoreincreases cardiomyocyte survival and viability 3.體內(nèi)研究 Dynasore ameliorates the motor dysfunction greatly at 3, 7, and 10 days after SCI in rats. Dynasoresignificantly enhances motor function which may be by inhibiting the

9、activation of neuronal mitochondrialapoptotic pathway and astrocytic proliferation in rats after SCI 4.PROTOCOLCell Assay 3 Mouse ventricular myocytes are isolated from male adult C6/Black mouse. Cardiomyocytes subjects to 2hours of drug treatment followed by oxidative stress (30 M H2O2 for 35 min).

10、 For ATP supplementexperiments, the cells are treated with 3 mM ATP for 30 min before exposure to H2O2. Cardiomyocytesurvival and viability are analyzed by trypan blue exclusion (TBE) assay 3.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Rats:

11、In the dynasore groups, the rats are given dynasore immediately at a dose of 1, 10, or 30 mg/kgAdministration 4 through intraperitoneal injection after SCI, while the rats in the sham and SCI groups receive DMSO (samevolume as dynasore groups) through intraperitoneal injection 4.MCE has not independ

12、ently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) J Am Chem Soc. 2018 Dec 12;140(49):17234-17240. Oncogene. 2018 Jan 4;37(1):116-127. Drug Deliv. 2018 Nov;25(1):1066-1079. Arab J Chem. 28 June 2018. Eur J Cell Biol. 2019 Jan;98(1):36-50.2/3 Master of Small Molecu

13、les 您邊的抑制劑師www.MedChemESee more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Macia E, et al. Dynasore, a cell-permeable inhibitor of dynamin. Dev Cell. 2006 Jun;10(6):839-50.2. Mues MB, et al. Dynasore disrupts trafficking of herpes simplex virus proteins. J Virol. 2015 Jul;89(13):66

14、73-84.3. Gao D, et al. Dynasore protects mitochondria and improves cardiac lusitropy in Langendorff perfused mouse heart. PLoS One. 2013 Apr15;8(4):e60967.4. Li G, et al. Dynasore Improves Motor Function Recovery via Inhibition of Neuronal Apoptosis and Astrocytic Proliferation after SpinalCord Injury in Rats. Mol Neurobiol. 2