Emetine (hydrochloride) |
| رقم الكتالوجGC43599 |
An anti-protozoal drug used for intestinal and tissue amoebiasis
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 316-42-7
Sample solution is provided at 25 µL, 10mM.
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Emetine (dihydrochloride) is an anti-protozoal drug previously used for intestinal and tissue amoebiasis[1].
Emetine dihydrochloride 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 isolates and IC50 values of 47 nM and 2.6 nM established for emetine dihydrochloride hydrate and DHA, respectively[1]. After the lymphoblasts are treated with emetine dihydrochloride, the expression level of the mutant allele is elevated almost equally to the wild-type alleles by direct sequencing of the corresponding cDNA[2]. Emetine dihydrochloride is identified as a lead compound with significant concentration dependent suppression of PEDF-induced TNF secretion and an IC50 of 146 nM. Emetine dihydrochloride inhibits PEDF-mediated TNF release without affecting cell viability and binds to PEDF receptor ATGL with high-binding affinity (KD=14.3 nM)[3].Emetine dihydrochloride reduces cell viability, induces apoptosis, promptes AML cells towards differentiation and downregulates HIF-1α[4].
Emetine dihydrochloride (0.002, 0.02, 0.2 and 2 mg/kg) not only attenuates blood glucose levels in dose-dependent way but also induces a persistent attenuation of blood glucose levels. Daily administration of emetine dihydrochloride dose-dependently attenuates hyperglycemic response by d 21. Consistent with this observation, administration of emetine dihydrochloride, but not the vehicle control, results in a sustained attenuation of blood glucose levels. Emetine dihydrochloride improves disease severity in a spontaneous model of NOD T1D[3]. Emetine dihydrochloride (1 mg/kg) reduces both leukemia burden in an in vivo xenotransplantation mouse model and the clonogenic capacity of leukemic cells upon treatment[4].
References:
[1]. Matthews H, et al. Drug repositioning as a route to anti-malarial drug discovery: preliminary investigation of the in vitro anti-malarial efficacy of emetine dihydrochloride hydrate. Malar J. 2013 Oct 9;12:359.
[2]. Wu L, et al. PRRT2 truncated mutations lead to nonsense-mediated mRNA decay in Paroxysmal Kinesigenic Dyskinesia. Parkinsonism Relat 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
| Cas No. | 316-42-7 | SDF | |
| Chemical Name | (2S,3R,11bS)-3-ethyl-1,3,4,6,7,11b-hexahydro-9,10-dimethoxy-2-[[(1R)-1,2,3,4-tetrahydro-6,7-dimethoxy-1-isoquinolinyl]methyl]-2H-benzo[a]quinolizine, dihydrochloride, hydrate | ||
| Canonical SMILES | CC[C@@H]1[C@@H](C[C@@]2(C3=CC(OC)=C(C=C3CCN2)OC)[H])C[C@]4(C5=CC(OC)=C(C=C5CCN4C1)OC)[H].Cl.Cl | ||
| Formula | C29H40N2O4 • 2HCl | M.Wt | 553.6 |
| الذوبان | 1mg/ml in chloroform; 100mg/ml in water | Storage | Store at -20°C,protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.8064 mL | 9.0318 mL | 18.0636 mL |
| 5 mM | 0.3613 mL | 1.8064 mL | 3.6127 mL |
| 10 mM | 0.1806 mL | 0.9032 mL | 1.8064 mL |
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 31 reference(s) in Google Scholar.)
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