Emetine (dihydrochloride hydrate)

7083-71-8

C29H40N2O4 . 2 HCl . H2O

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

Autophagy; Anti-infection

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 (K_D=14.3 nM)^[3]. Emetine treatment reduces cell viability, induces apoptosis, promptes AML cells towards differentiation and downregulates HIF-1alpha^[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].