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Oleandomycin

(Synonyms: 竹桃霉素) 目录号 : GC10095

A macrolide antibiotic

Oleandomycin Chemical Structure

Cas No.:3922-90-5

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产品描述

Oleandomycin is an antibiotic produced by strains of Streptomyces.

In vitro: Oleandomycin has been identified as a macrolide antibiotic demonstrating antimicrobial activity similar to penicillin and erythromycin. In addition, oleandomycin structurally has a macrocyclic lactone ring of 14 carbon atoms with one sugar, oleandrose, and one amino sugar, desoxamine [1].

In vivo: The PK of oleandomycin after i.v. and po administration, both alone and after i.m. pretreatment with metamizole or dexamethasone, was studied in healthy dogs. Results showed that after i.v. injection of oleandomycin alone at 10 mg/kg, the t1/2β, Vd, Cl and AUC were 1.60 h, 1.11 L/kg, 7.36 ml/kg/min and 21.66 μg h/ml, respectively. There were no statistically significant differences following pretreatment with metamizole or dexamethasone. In addition, after po administration of oleandomycin alone, the t1/2β, Cmax, tmax), MAT and Fabs were 1.68 h, 5.34 μg/ml, 1.5 h, 1.34 h and 84.29%, respectively, and the pretreatment with metamizole showed a significantly decreased value for Cmax but the MAT was increased significantly. Statistically significant changes in the PK parameters of oleandomycin following po administration were also seen as a result of pretreatment with dexamethasone. The Cmax was increased and the tmax and MAT were lower [2].

Clinical trial: Up to now, oleandomycin is still in the preclinical development stage.

References:
[1] C.  Vilches, C. Méndez, C. Hardisson, et al. Biosynthesis of oleandomycin by Streptomyces antibioticus: Influence of nutritional conditions and development of resistance. J.Gen.Microbiol. 136(8), 1447-1454 (1990).
[2] Milanova A, Lashev L.  Pharmacokinetics of oleandomycin in dogs after intravenous or oral administration alone and after pretreatment with metamizole or dexamethasone. Vet Res Commun. 2002 Jan;26(1):61-71.

Chemical Properties

Cas No. 3922-90-5 SDF
别名 竹桃霉素
化学名 7-(α-D-galactopyranosyloxy)-4-methyl-2H-1-benzopyran-2-one
Canonical SMILES O=C1[C@@H]([C@H]([C@H]([C@H](OC([C@@H]([C@H]([C@@H]([C@H]([C@H](C[C@@]12CO2)C)O[C@]3([C@@H]([C@H](C[C@H](O3)C)N(C)C)O)[H])C)O[C@@]4(O[C@H]([C@@H]([C@H](C4)OC)O)C)[H])C)=O)C)C)O)C
分子式 C35H61NO12 分子量 687.9
溶解度 DMF: Soluble,DMSO: Soluble,Ethanol: Soluble,Methanol: Soluble 储存条件 Store at -20°C
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1 mM 1.4537 mL 7.2685 mL 14.537 mL
5 mM 0.2907 mL 1.4537 mL 2.9074 mL
10 mM 0.1454 mL 0.7268 mL 1.4537 mL
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