Name | emetine |
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Synonyms |
EMETINE
Emetine hydrochloride (2S,3R,11bS)-2-[[(1R)-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolin-1-yl]methyl]-3-ethyl-9,10-dimethoxy-2,3,4,6,7,11b-hexahydro-1H-benzo[a]quinolizine Emetine [BAN] Emetin Cephaline-O-methyl ether Emetan,6',7',10,11-tetramethoxy 10,11,6',7'-tetramethoxy-emetane Methyl cephaeline Cephaeline methyl ether |
Description | Emetine is an anti-protozoal drug previously used for intestinal and tissue amoebiasis[1]. |
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Related Catalog | |
In Vitro | Emetine 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 and DHA, respectively[1]. After the lymphoblasts are treated with emetine, 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 and binds to PEDF receptor ATGL with high-binding affinity (KD=14.3 nM)[3]. Emetine 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) 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]. |
References |
Density | 1.17g/cm3 |
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Boiling Point | 600.3ºC at 760mmHg |
Melting Point | 89-96ºC |
Molecular Formula | C29H40N2O4 |
Molecular Weight | 517.10000 |
Flash Point | 316.9ºC |
Exact Mass | 516.27500 |
PSA | 52.19000 |
LogP | 6.01210 |
CHEMICAL IDENTIFICATION
HEALTH HAZARD DATAACUTE TOXICITY DATA
MUTATION DATA
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RIDADR | UN 1544 |
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Packaging Group | III |
Hazard Class | 6.1(b) |