Dirithromycin

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Chemical Structure| 62013-04-1 同义名 : LY237216;Antibiotic AS-E 136
CAS号 : 62013-04-1
货号 : A612277
分子式 : C42H78N2O14
纯度 : 98%
分子量 : 835.074
MDL号 : MFCD00865041
存储条件：

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

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
动物实验配方：
生物活性
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].
临床研究
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 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.20mL

0.24mL

0.12mL

5.99mL

1.20mL

0.60mL

11.97mL

2.39mL

1.20mL
参考文献

[1]Arda B, Tuncel M, et al. Efficacy of oral levofloxacin and dirithromycin alone and in combination with rifampicin in the treatment of experimental murine Brucella abortus infection. Int J Antimicrob Agents. 2004 Feb;23(2):204-7.

[2]Moutard I, Gressier B, et al. In vitro effects of spiramycin and dirithromycin on IL1 beta production by human LPS-stimulated mononuclear cells. Therapie. 1999 Sep-Oct;54(5):607-12.

[3]Brogden RN, Peters DH. Dirithromycin. A review of its antimicrobial activity, pharmacokinetic properties and therapeutic efficacy. Drugs. 1994;48(4):599‐616.

[4]Wintermeyer SM, Abdel-Rahman SM, Nahata MC. Dirithromycin: a new macrolide. Ann Pharmacother. 1996;30(10):1141‐1149.

[5]Sides GD, Cerimele BJ, Black HR, Busch U, DeSante KA. Pharmacokinetics of dirithromycin. J Antimicrob Chemother. 1993;31 Suppl C:65‐75.

[6]Hand WL, Hand DL. Interactions of dirithromycin with human polymorphonuclear leukocytes. Antimicrob Agents Chemother. 1993;37(12):2557‐2562.