Emetine-dihydrochloride-hydrate-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEEmetine dihydrochloride hydrateCat. No.: HY-B1479BCAS No.: 7083-71-8分式: CHNO . HCl . HO分量: 571.58作靶點: Parasite; Autophagy作通路: Anti-infection; Autophagy儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外

2、實驗 DMSO : 16.5 mg/mL (28.87 mM; Need ultrasonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 1.7495 mL 8.7477 mL 17.4954 mL5 mM 0.3499 mL 1.7495 mL 3.4991 mL10 mM 0.1750 mL 0.8748 mL 1.7495 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Emetine dihydrochloride

3、 hydrate種抗原藥，早期于治療腸道和組織的阿巴病。體外研究Emetine dihydrochloride hydrate is reported to have an IC50 value of 1 nM on the drug sensitive 3D7 P.falciparum parasite strains. Dose response curves are determined for both drugs using K1 resistant isolatesand IC50 values of 472.1 nM and 2.60.41 nM established for

4、emetine dihydrochloride hydrate and DHA,respectively 1. After the lymphoblasts are treated with cycloheximide or emetine dihydrochloride hydrate,the expression level of the mutant allele is elevated almost equally to the wild-type alleles by direct1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEseq

5、uencing of the corresponding cDNA 2. Emetine is identified as a lead compound with significantconcentration dependent suppression of PEDF-induced TNF secretion and an IC50 of 146 nM. Emetineinhibits PEDF-mediated TNF release without affecting cell viability. Emetine binds to PEDF receptor ATGLwith h

6、igh-binding affinity (KD=14.3 nM) 3. Emetine treatment reduces cell viability, induces apoptosis,promptes AML cells towards differentiation and downregulates HIF-1 4.體內(nèi)研究 Emetine (0.002, 0.02, 0.2 and 2 mg/kg) does not induce any significant difference in body weight in mice withlow-dose streptozoto

7、cin model of T1D. Administration of emetine not only attenuates blood glucose levels indose-dependent way but also induces a persistent attenuation of blood glucose levels. Daily administration ofemetine dose-dependently attenuates hyperglycemic response by d 21. Consistent with this observation,adm

8、inistration of emetine, but not the vehicle control, results in a sustained attenuation of blood glucoselevels. Emetine improves disease severity in a spontaneous model of NOD T1D 3. Emetine (1 mg/kg)reduces both leukemia burden in an in vivo xenotransplantation mouse model and the clonogenic capaci

9、ty ofleukemic cells upon treatment 4.PROTOCOLCell Assay 4 7.5105 cells per mL are cultured in 96-well plates in complete medium. Emetine and Ara-C are added atindicated concentrations. Cell viability is measured by 7-AAD exclusion and Hoechst33342 positivity stainingby flow cytometry; and cell count

10、 is obtained by volume in a FACSCantoII cytometer. Statistical analysis andEC50 determination are calculated in GraphPad. FlowJo software is used for flow cytometry analysis.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal T1D is induced by admini

11、stration of streptozotocin (50 mg/kg dissolved in sodium citrate buffer, pH 4.5) to 6Administration 3 to 8 wk old C57Bl/6 mice intraperitoneally (i.p.) once each day for 5 consecutive days. Mice are given watersupplemented with 10% sucrose for six days to prevent sudden hypoglycemia during streptozo

12、tocinadministration. For time course studies, body weight and blood glucose are measured every other day. Bloodglucose is measured with a FreeStyle Lite blood glucose meter. For studies with emetine, mice receive dailyadministration of emetine dihydrochloride (0.002, 0.02, 0.2 and 2 mg/kg) or saline

13、. Blood glucose with eitherFreeStyle Lite blood glucose meter or Bayer Contour blood glucose meter and body weight are measuredonce weekly. At the end of each study, mice are euthanized by CO2 asphyxiation. Blood and pancreas arecollected for cytokine analysis.MCE has not independently confirmed the

14、 accuracy of these methods. They are for reference only.REFERENCES1. Matthews H, et al. Drug repositioning as a route to anti-malarial drug discovery: preliminary investigation of the in vitro anti-malarialefficacy of emetine dihydrochloride hydrate. Malar J. 2013 Oct 9;12:359.2. Wu L, et al. PRRT2

15、truncated mutations lead to nonsense-mediated mRNA decay in Paroxysmal Kinesigenic Dyskinesia. ParkinsonismRelat Disord. 2014 Dec;20(12):1399-404.3. Hudson LK, et al. Emetine Di-HCl attenuates Type 1 diabetes mellitus in mice. Mol Med. 2016 Jun 10;22.4. Cornet-Masana JM, et al. Emetine induces chemosensitivity and reduces clonogenicity of acute myeloid leukemia cells. Oncotarget.2016 Apr 26;7(17):23239-50.2/3 Master of Smal