货号:A612277
同义名:
LY237216; Antibiotic AS-E 136
Dirithromycin是一种红霉素衍生物,属于半合成大环内酯类抗生素,具有口服活性。该化合物对革兰氏阳性菌、军团菌属(Legionella spp.)、幽门螺杆菌(Helicobacter pylori)和沙眼衣原体(Chlamydia trachomatis)均表现出抑制活性,常用于相关微生物感染机制的研究。


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| 描述 | Dirithromycin is a new macrolide with a spectrum and degree of in vitro antimicrobial activity similar to that of erythromycin. Multicentre double-blind clinical trials have shown dirithromycin to be similar in efficacy to erythromycin in the treatment of uncomplicated bacterial infections of the respiratory tract and of skin and soft tissues[3]. Dirithromycin offers some attractive pharmacokinetic properties. The long elimination half-life of dirithromycin allows once-daily dosing and higher and more prolonged tissue concentrations than are achievable with erythromycin[4]. Dirithromycin achieves relatively high tissue concentrations (approximately 0.8 - 5.0 mg/kg) 4 - 24 h after dosing[5]. The presence of dirithromycin slightly increased the intraphagocytic killing of Staphylococcus aureus in human PMNs (polymorphonuclear leukocytes)[6]. |
| Concentration | Treated Time | Description | References | |
| Thermus thermophilus 70S ribosome | 250 μM | To study the binding mode of Dirithromycin to the 70S ribosome, revealing a unique interaction between its side chain and the His69 residue of ribosomal protein uL4 | Antimicrob Agents Chemother. 2019 May 24;63(6):e02266-18 | |
| 3T3 mouse fibroblast cell lines | 0.25 μg/mL | 24 and 48 hours | Evaluated cytotoxicity, cell viability was 83.36% and 63.36% at highest concentration | Turk J Pharm Sci. 2017 Aug;14(2):191-200 |
| Escherichia coli 70S ribosome | 30 µM | 5 minutes | To study the binding mode of Dirithromycin to the ribosome and its inhibitory effect on protein synthesis | RNA. 2020 Jun;26(6):715-723 |
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT02237768 | Healthy | Phase 1 | Unknown | December 2014 | Jordan ... 展开 >> Arab Pharmaceutical industry Consulting/ Pharmaceutical Research Unit Not yet recruiting Amman, Jordan, 11941 Principal Investigator: Rana T Bustami, Ph.D. Pharmacy 收起 << |
| NCT02185846 | Healthy | Phase 1 | Completed | - | Jordan ... 展开 >> Arab Pharmaceutical industry Consulting/ Pharmaceutical Research Unit Amman, Jordan, 11941 收起 << |
| NCT02185833 | Healthy | Phase 1 | Completed | - | Jordan ... 展开 >> Arab Pharmaceutical industry Consulting/ Pharmaceutical Research Unit Amman, Jordan, 11941 收起 << |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
1.20mL 0.24mL 0.12mL |
5.99mL 1.20mL 0.60mL |
11.98mL 2.40mL 1.20mL |
|
| CAS号 | 62013-04-1 |
| 分子式 | C42H78N2O14 |
| 分子量 | 835.07 |
| SMILES Code | CC1[C@@]([C@](O)([C@H](OC([C@@H]2C)=O)CC)C)([H])O[C@H](COCCOC)N[C@@]1([H])[C@](C[C@@](O)([C@@H]([C@@H](C)[C@]2([H])O[C@@](O[C@@H](C)[C@@H]3O)([H])C[C@@]3(C)OC)O[C@@](O[C@H](C)C[C@@H]4N(C)C)([H])[C@@H]4O)C)([H])C |
| MDL No. | MFCD00865041 |
| 别名 | LY237216; Antibiotic AS-E 136 |
| 运输 | 蓝冰 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Sealed in dry, 2-8°C |
| 溶解方案 |
DMSO: 35 mg/mL(41.91 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 无水乙醇: 50 mg/mL(59.87 mM),注意:无水乙醇开封后,易挥发,也会吸收空气中的水分,导致溶解能力下降,请避免使用开封较久的乙醇 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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