Name | Sigapedil |
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Synonyms |
erythroped
Refkas erythromycin gluceptate Monomycin erythromycin ethyl succinate D-Glucoheptonat erythromycin A 2'-ethyl succinate Erythromycin glucoheptonate Evesin Erythromycin-A,D-glycero-D-gulo-Heptonat Eryliquid Anamycin E-Mycin e Esinol O''-(3-ethoxycarbonyl-propionyl)-erythromycin erythromycin-A,D-glycero-D-gulo-heptonate Erythromycinethylsuccinat Arpimycin |
Description | Erythromycin gluceptate is a macrolide antibiotic produced by actinomycete Streptomyces erythreus with a broad spectrum of antimicrobial activity. Erythromycin gluceptate binds to bacterial 50S ribosomal subunits and inhibits RNA-dependent protein synthesis by blockage of transpeptidation and/or translocation reactions, without affecting synthesis of nucleic acid[1][2]. Erythromycin gluceptate also exhibits antitumor and neuroprotective effect in different fields of research[3][4]. |
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Related Catalog | |
Target |
Bacterial; RNA-dependent protein synthesis[1] |
In Vitro | Erythromycin gluceptate inhibits growth of P. falciparum with IC50 and IC90 values of 58.2 μM and 104.0 μM, respectively[1]. Erythromycin gluceptate (10 μM, 100 μM; 24 h, 72 h) shows antioxidant and anti-inflammatory effects and suppresses the accumulation of 4-HNE (p<0.01) and 8-OHdG (p<0.01), reduces Iba-1 (p<0.01) and TNF-α (p<0.01) expression significantly[4]. Cell Viability Assay[4] Cell Line: Embryos primary cortical neuron (from the cerebral cortices of 17-day-old Sprague-Dawley rat) Concentration: 10, 100 μM Incubation Time: 24, 72 hours Result: Improved the viability of cultured neuronal cells in vitro after 3 hours oxygen-glucose deprivation (OGD). |
In Vivo | Erythromycin gluceptate (gastric intubation; 0.1-50 mg/kg; 30-120 days) decreases tumor growth and prolong the survival time of mice from dose of 5 mg/kg in mice[3]. Erythromycin gluceptate (gastric intubation; 5 mg/kg) protects mice alive even at 120 days after inoculation, but shortens mean survival time in tumor-bearing mice by 4-5 days with dose of 50 mg/kg[3]. Erythromycin gluceptate (i.h.; single injection; 50 mg/kg) has a protective effect on the rat model with cerebral ischemia reperfusion-injury[4]. Animal Model: Female ddY mice (6-week-old) with EAC cells or CDF mice (6-week-old) with P388 cells[3] Dosage: 0.1 mg/kg; 0.5 mg/kg; 10 mg/kg; 30 mg/kg; 50 mg/kg Administration: Gastric intubation; 30-120 days Result: Decreased tumor growth and prolonged the mean survival time of mice from the dose of 5 mg/kg, however, the 50 mg/kg dosage shortened the MST in tumorbearing mice. Animal Model: Male Sprague-Dawley rats (8-week-old, 250-300 g)[4] Dosage: 50 mg/kg Administration: Subcutaneous single injection Result: Reduced infarct volume and edema volume, improved neurological deficit. |
References |
[1]. Gribble MJ, et al. Erythromycin. Med Clin North Am. 1982 Jan;66(1):79-89. [3]. K Hamada, et al. Antitumor effect of erythromycin in mice. Chemotherapy. 1995 Jan-Feb. 41(1):59-69. |
Boiling Point | 818.4ºC at 760 mmHg |
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Molecular Formula | C44H81NO21 |
Molecular Weight | 960.10800 |
Flash Point | 448.8ºC |
Exact Mass | 959.53000 |
PSA | 352.59000 |
Vapour Pressure | 4.94E-31mmHg at 25°C |
RIDADR | NONH for all modes of transport |
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