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  3. Emetine dihydrochloride hydrate

Emetine dihydrochloride hydrate 

Cat. No.: HY-B1479B Purity: 98.48%
Handling Instructions

Emetine dihydrochloride hydrate is an anti-protozoal drug previously used for intestinal and tissue amoebiasis.

For research use only. We do not sell to patients.

Emetine dihydrochloride hydrate Chemical Structure

Emetine dihydrochloride hydrate Chemical Structure

CAS No. : 7083-71-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
10 mg USD 60 In-stock
Estimated Time of Arrival: December 31
50 mg USD 108 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Emetine dihydrochloride hydrate is an anti-protozoal drug previously used for intestinal and tissue amoebiasis.

In Vitro

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 isolates and IC50 values of 47±2.1 nM and 2.6±0.41 nM established for 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 direct sequencing of the corresponding cDNA[2]. Emetine is identified as a lead compound with significant concentration dependent suppression of PEDF-induced TNF secretion and an IC50 of 146 nM. Emetine inhibits PEDF-mediated TNF release without affecting cell viability. Emetine binds to PEDF receptor ATGL with high-binding affinity (KD=14.3 nM)[3]. Emetine treatment reduces cell viability, induces apoptosis, promptes AML cells towards differentiation and downregulates HIF-1α[4].

In Vivo

Emetine (0.002, 0.02, 0.2 and 2 mg/kg) does not induce any significant difference in body weight in mice with low-dose streptozotocin model of T1D. Administration of emetine not only attenuates blood glucose levels in dose-dependent way but also induces a persistent attenuation of blood glucose levels. Daily administration of emetine dose-dependently attenuates hyperglycemic response by d 21. Consistent with this observation, administration of emetine, but not the vehicle control, results in a sustained attenuation of blood glucose levels. 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 capacity of leukemic cells upon treatment[4].

Molecular Weight

571.58

Formula

C₂₉H₄₀N₂O₄ . ₂ HCl . H₂O

CAS No.

7083-71-8

SMILES

CC[[email protected]@H]1[[email protected]](C[[email protected]@]2([H])C3=CC(OC)=C(OC)C=C3CCN2C1)C[[email protected]]4([H])C5=CC(OC)=C(OC)C=C5CCN4.[H]Cl.[H]Cl.O

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 16.5 mg/mL (28.87 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7495 mL 8.7477 mL 17.4954 mL
5 mM 0.3499 mL 1.7495 mL 3.4991 mL
10 mM 0.1750 mL 0.8748 mL 1.7495 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[4]

7.5×105 cells per mL are cultured in 96-well plates in complete medium. Emetine and Ara-C are added at indicated concentrations. Cell viability is measured by 7-AAD exclusion and Hoechst33342 positivity staining by flow cytometry; and cell count is obtained by volume in a FACSCantoII cytometer. Statistical analysis and EC50 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 Administration
[3]

T1D is induced by administration of streptozotocin (50 mg/kg dissolved in sodium citrate buffer, pH 4.5) to 6 to 8 wk old C57Bl/6 mice intraperitoneally (i.p.) once each day for 5 consecutive days. Mice are given water supplemented with 10% sucrose for six days to prevent sudden hypoglycemia during streptozotocin administration. For time course studies, body weight and blood glucose are measured every other day. Blood glucose is measured with a FreeStyle Lite blood glucose meter. For studies with emetine, mice receive daily administration of emetine dihydrochloride (0.002, 0.02, 0.2 and 2 mg/kg) or saline. Blood glucose with either FreeStyle Lite blood glucose meter or Bayer Contour blood glucose meter and body weight are measured once weekly. At the end of each study, mice are euthanized by CO2 asphyxiation. Blood and pancreas are collected for cytokine analysis.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: 98.48%

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Emetine dihydrochloride hydrate
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