Erythromycin estolate
(Synonyms: 依托红霉素) 目录号 : GC39662
Erythromycin (Lubomycine B), a naturally occurring macrolide, is derived from Streptomyces erythrus. It inhibits bacterial protein synthesis by binding to bacterial 50S ribosomal subunits.
Cas No.:3521-62-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Erythromycin (Lubomycine B), a naturally occurring macrolide, is derived from Streptomyces erythrus. It inhibits bacterial protein synthesis by binding to bacterial 50S ribosomal subunits.
| Cas No. | 3521-62-8 | SDF | |
| 别名 | 依托红霉素 | ||
| Canonical SMILES | CCCCCCCCCCCCOS(=O)(O)=O.CCC(O[C@H]([C@H](C[C@@H](C)O1)N(C)C)[C@]1([H])O[C@@H]2[C@H]([C@@H]([C@H](C(O[C@@H]([C@@](C)(O)[C@H](O)[C@@H](C)C([C@H](C)C[C@]2(O)C)=O)CC)=O)C)O[C@@]3([H])C[C@](C)([C@@H](O)[C@H](C)O3)OC)C)=O | ||
| 分子式 | C52H97NO18S | 分子量 | 1056.39 |
| 溶解度 | DMSO: 250 mg/mL (236.66 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 0.9466 mL | 4.7331 mL | 9.4662 mL |
| 5 mM | 0.1893 mL | 0.9466 mL | 1.8932 mL |
| 10 mM | 0.0947 mL | 0.4733 mL | 0.9466 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Erythromycin estolate Is a Potent Inhibitor Against HCoV-OC43 by Directly Inactivating the Virus Particle
Front Cell Infect Microbiol 2022 Jul 7;12:905248.PMID:35873167DOI:10.3389/fcimb.2022.905248.
In addition to antibacterial effects, macrolide antibiotics exhibit other extensive pharmacological effects, such as anti-inflammatory and antiviral activities. Erythromycin estolate, one of the macrolide antibiotics, was previously investigated to effectively inhibit infections of various flaviviruses including Zika virus, dengue virus, and yellow fever virus, but its antiviral effect against human coronavirus remains unknown. Thus, the current study was designed to evaluate the antiviral efficacy of Erythromycin estolate against human coronavirus strain OC43 (HCoV-OC43) and to illustrate the underlying mechanisms. Erythromycin estolate effectively inhibited HCoV-OC43 infection in different cell types and significantly reduced virus titers at safe concentration without cell cytotoxicity. Furthermore, Erythromycin estolate was identified to inhibit HCoV-OC43 infection at the early stage and to irreversibly inactivate virus by disrupting the integrity of the viral membrane whose lipid component might be the target of action. Together, it was demonstrated that Erythromycin estolate could be a potential therapeutic drug for HCoV-OC43 infection.
Erythromycin estolate and jaundice
Br Med J (Clin Res Ed) 1983 Jun 18;286(6382):1954-5.PMID:6407653DOI:10.1136/bmj.286.6382.1954.
Using prescription-event monitoring to determine whether Erythromycin estolate was a more frequent cause of jaundice than erythromycin stearate or tetracycline 12 208 patients, for whom 5343 doctors had prescribed one of the three drugs, were identified by the Prescription Pricing Authority. Of the questionnaires sent to general practitioners about the possible occurrence of jaundice, 76% were returned. There were 16 reports of jaundice, of which four were attributable to gall stones, three to cancer, six to viral hepatitis, and only three were possibly related to an antibiotic. All three patients, in whom the antibiotic was a possible cause, had been treated with erythromycin stearate. No case was attributable to the estolate which had previously been suspected of being a more frequent cause of jaundice. Although the incidence is unknown, it is very unlikely to be more than one in 100.
Pharmacokinetics of Erythromycin estolate and erythromycin phosphate after intragastric administration to healthy foals
Am J Vet Res 2000 Aug;61(8):914-9.PMID:10951982DOI:10.2460/ajvr.2000.61.914.
Objective: To determine pharmacokinetics and plasma concentrations of erythromycin and related compounds after intragastric administration of erythromycin phosphate and Erythromycin estolate to healthy foals. Animals: 11 healthy 2- to 6-month-old foals. Procedure: Food was withheld from foals overnight before intragastric administration of Erythromycin estolate (25 mg/kg of body weight; n = 8) and erythromycin phosphate (25 mg/kg; 7). Four foals received both drugs with 2 weeks between treatments. Plasma erythromycin concentrations were determined at various times after drug administration by use of high-performance liquid chromatography. Maximum plasma peak concentrations, time to maximum concentrations, area under plasma concentration versus time curves, half-life of elimination, and mean residence times were determined from concentration versus time curves. Results: Maximum peak concentration of erythromycin A after administration of erythromycin phosphate was significantly greater than after administration of Erythromycin estolate (2.9 +/- 1.1 microg/ml vs 1.0 +/- 0.82 microg/ml). Time to maximum concentration was shorter after administration of erythromycin phosphate than after Erythromycin estolate (0.71 +/- 0.29 hours vs 1.7 +/- 1.2 hours). Concentrations of anhydroerythromycin A were significantly less 1 and 3 hours after administration of Erythromycin estolate than after administration of erythromycin phosphate. Conclusions and clinical relevance: Plasma concentrations of erythromycin A remained > 0.25 microg/ml (reported minimum inhibitory concentration for Rhodococcus equi) for at least 4 hours after intragastric administration of erythromycin phosphate or Erythromycin estolate, suggesting that the recommended dosage for either formulation (25 mg/kg, q 6 h) should be adequate for treatment of R equi infections in foals.
Erythromycin estolate impairs the mitochondrial and microsomal calcium homeostasis: correlation with hepatotoxicity
Arch Toxicol Suppl 1984;7:298-302.PMID:6595996DOI:10.1007/978-3-642-69132-4_49.
The effects of Erythromycin estolate, a well known hepatotoxic macrolide antibiotic, on isolated rat hepatocyte viability and on subcellular Ca2+ transport have been investigated. Erythromycin estolate (0.5 mM), but not erythromycin base and erythromycin ethylsuccinate, induced 100% cell death after 60 min incubation, and caused maximal inhibition of mitochondrial and microsomal Ca2+ sequestration activities at 0.1 mM concentration. Sodium lauryl sulphate, which is the surfactant moiety of the Erythromycin estolate molecule, caused effects similar to those exhibited by Erythromycin estolate. Disorders of the intracellular calcium homeostasis seem to play a role in the lauryl sulphate-mediated hepatotoxic action of Erythromycin estolate.
Pharmacokinetic advantages of Erythromycin estolate over ethylsuccinate as determined by high-pressure liquid chromatography
Antimicrob Agents Chemother 1988 Apr;32(4):561-5.PMID:3259856DOI:10.1128/AAC.32.4.561.
The pharmacokinetics of Erythromycin estolate (500 mg) and erythromycin ethylsuccinate (600 mg) were compared in 12 healthy volunteers after single doses and after repeated oral doses (every 8 h). High-pressure liquid chromatography with electrochemical detection was used to determine concentrations in plasma and urine of estolate, ethylsuccinate, and erythromycin base. The maximum concentration of drug in the serum, the half-life, and the area under the curve for Erythromycin estolate were significantly greater than those of erythromycin ethylsuccinate after both regimens. After single and multiple doses, the respective areas under the curve of erythromycin base generated by estolate formulation were 3 and 1.6 times greater (P less than 0.05) than those of ethylsuccinate. The lower percentage of hydrolysis of Erythromycin estolate (41 versus 69%) combined with its longer half-life (5.47 versus 2.72 h) and its larger area under the curve (30.61 versus 4.68 micrograms/h/ml, after multiple doses) could explain these differences. This study underscores the need for a specific high-pressure liquid chromatography assay and the importance of wide variability, rate-limited processes, changes with multiple doses, and the appearance of a second peak when one studies the pharmacokinetics of erythromycin esters. The pharmacokinetic data presented in this study reinforce the clinical advantages of Erythromycin estolate over erythromycin ethylsuccinate.