交沙霉素

作用适应症检测方法生物活性靶点体外研究体内研究交沙霉素试剂级价格

交沙霉素

CAS号:16846-24-5
英文名:Josamycin
中文名:交沙霉素
CBNumber:CB5444692
分子式:C42H69NO15
分子量:827.99
MOL File:16846-24-5.mol

交沙霉素化学性质

熔点 :131.5℃
比旋光度 :D25 -70° (c = 1 in ethanol)
沸点 :763.27°C (rough estimate)
密度 :1.1547 (rough estimate)
折射率 :1.6220 (estimate)
储存条件 :Inert atmosphere,Store in freezer, under -20°C
溶解度 :Soluble in ethanol
酸度系数(pKa) :7.1 (40% aq methanol)
形态 :powder
颜色 :white to slightly yellow
Merck :13,5286
稳定性 :Hygroscopic

安全信息

WGK Germany :2
RTECS号 :OH4725810
F :10
毒性 :LD50 oral in rat: > 7gm/kg

交沙霉素化学药品说明书

交沙霉素颗粒剂
交沙霉素胶囊

交沙霉素性质、用途与生产工艺

作用抗菌作用与红霉素相似。对革兰阳性菌如金黄色葡萄球菌、溶血性链球菌、肺炎球菌、白喉杆菌、破伤风杆菌、炭疽杆菌等均有抗菌作用，对部分革兰阴性菌如淋球菌、百日咳杆菌、布鲁菌等也有作用，对支原体、衣原体、立克次体和螺旋体等有效，对弯曲杆菌属、军团菌也敏感，对革兰阳性厌氧菌较红霉素更为有效。
适应症临床主要用敏感菌所致呼吸系、胆道感染、化脓性皮肤病、中耳炎、鼻窦炎、扁桃体炎、牙周脓肿等。亦可用对青霉素、红霉素耐药的葡萄球菌感染。
检测方法交沙霉素效价的生物检测法主要采用管碟法。管碟法利用抗生素在琼脂培养基中的扩散作用，将己知浓度的标准溶液和未知浓度的样品在含有敏感性实验菌的琼脂表面进行扩散，由于对被试菌的抑制作用而产生抑菌圈，抑菌圈的大小和抗生素的浓度间有一比例。这个方法利用抗生素抑制敏感菌的特点，符合临床使用的实际情况，因此被国际公认。
生物活性 Josamycin (EN-141, Kitasamycin A3, Leucomycin A3, Turimycin A5)是一种来源于那波链霉菌的大环内脂类抗菌素，对一系列的病原体具有广泛的抗菌活性。
靶点

Kd: 5.5 nM (ribosome)
体外研究

Studies show that the average lifetime on the ribosome is 3 h for Josamycin and that the dissociation constants for Josamycin binding to the ribosome is 5.5 nM. Josamycin slows down formation of the first peptide bond of a nascent peptide in an amino acid-dependent way and completely inhibits formation of the second or third peptide bond, depending on peptide sequence at a saturating drug concentration, synthesis of fulllength proteins is completely shut down by Josamycin. At a saturating drug concentration, synthesis of fulllength proteins is completely shut down by Josamycin.
体内研究

Blood and tissue levels of Josamycin after oral administration are 200 mg/kg to rabbits. Tissue levels are generally much higher than the blood levels, and 3 h after the administration, when the blood level is very low, the tissue levels are rather higher than those 1 h after the dose. One hour after the medication, the level in the lungs is the highest of all the tissue levels.