品牌现货直购
供应商:我要出现这里








查看所有供应商和价格请点击:

16846-24-5生产厂家

16846-24-5价格

16846-24-5

16846-24-5结构式
16846-24-5结构式
  • 常用中文名:交沙霉素
  • 常用英文名:Josamycin
  • CAS号:16846-24-5
  • 分子式:C42H69NO15
  • 分子量:827.995
  • 相关类别: 原料药 抗生素类药物 大环内酯类药
  • 发布时间:2018-02-12 08:00:00
  • 更新时间:2024-01-02 14:42:19
  • Josamycin (EN-141) 是一种大环内酯类抗生素,对多种病原体, 比如细菌 (bacteria) 具有抗菌活性。 Josamycin (EN-141) 对核糖体的解离常数 Kd 为 5.5 nM。

化源商城直购

中文名 交沙霉素
英文名 josamycin
中文别名 角沙霉素
英文别名 (2S,3R,4R,6S)-6-{[(2R,3S,4R,5R,6S)-6-{[(4R,6S,7R,9R,10R,11E,13E,16R)-4-Acetoxy-10-hydroxy-5-methoxy-9,16-dimethyl-2-oxo-7-(2-oxoethyl)oxacyclohexadeca-11,13-dien-6-yl]oxy}-4-(dimethylamino)-5-hydroxy-2-methyltetrahydro-2H-pyran-3-yl]oxy}-4-hydroxy-2,4-dimethyltetrahydro-2H-pyran-3-yl 3-methylbutanoate
Iosalide
4-(acetyloxy)-6-((3,6-dideoxy-4-O-(2,6-dideoxy-3-C-methyl-4-O-(3-methyl-1-oxobutyl)-α-L-ribo-hexopyranosyl)-3-(dimethylamino)-β-D-glucopyranosyl)oxy)-10-hydroxy-5-methoxy-9,16-dimethyl-2-oxooxacyclohexadeca-11,13-diene-7-acetaldehyde
Vilprafen
Leucomycin V 3-Acetate 4B-(3-Methylbutanoate)
MFCD00211043
Leucomycin A3
EN 141
Josamina
EINECS 240-871-6
JOSAMYCIN
carbomycin B
Jomybel
(2S,3R,4R,6S)-6-{[(2R,3S,4R,5R,6S)-6-{[(4R,6S,7R,9R,10R,11E,13E,16R)-4-(acetyloxy)-10-hydroxy-5-methoxy-9,16-dimethyl-2-oxo-7-(2-oxoethyl)oxacyclohexadeca-11,13-dien-6-yl]oxy}-4-(dimethylamino)-5-hydroxy-2-methyltetrahydro-2H-pyran-3-yl]oxy}-4-hydroxy-2,4-dimethyltetrahydro-2H-pyran-3-yl 3-methylbutanoate (non-preferred name)
YL-704A3
Wilprafen
Josacine
(2S,3R,4R,6S)-6-{[(2R,3S,4R,5R,6S)-6-{[(4R,6S,7R,9R,10R,11E,13E,16R)-4-Acetoxy-10-hydroxy-5-methoxy-9,16-dimethyl-2-oxo-7-(2-oxoethyl)oxacyclohexadeca-11,13-dien-6-yl]oxy}-4-(dimethylamino)-5-hydroxy-2-methyltetrahydro-2H-pyran-3-yl]oxy}-4-hydroxy-2,4-dimethyltetrahydro-2H-pyran-3-yl 3-methylbutanoate (non-preferred name)
描述 Josamycin (EN-141) 是一种大环内酯类抗生素,对多种病原体, 比如细菌 (bacteria) 具有抗菌活性。 Josamycin (EN-141) 对核糖体的解离常数 Kd 为 5.5 nM。
相关类别
靶点

Kd: 5.5 nM (ribosome)[1]

体外研究 研究表明,对于交沙霉素,核糖体的平均寿命为3小时,并且Josamycin与核糖体结合的解离常数为5.5nM。交沙霉素以氨基酸依赖性方式减慢新生肽的第一个肽键的形成,并完全抑制第二个或第三个肽键的形成,这取决于饱和药物浓度下的肽序列,全长蛋白质的合成完全关闭由Josamycin提供。在饱和药物浓度下,全长蛋白质的合成被Josamycin完全关闭[1]。
体内研究 口服给药后交沙霉素的血液和组织水平为兔子200mg/kg。组织水平通常远高于血液水平,并且在给药后3小时,当血液水平非常低时,组织水平相当高于给药后1小时的组织水平。服药一小时后,肺部水平是所有组织水平中最高的[2]。
激酶实验 在多晶缓冲液中制备交沙霉素,其含有5mM乙酸镁,5mM氯化铵,95mM氯化钾,0.5mM氯化钙,8mM腐胺,1mM亚精胺,5mM磷酸钾和1mM二硫赤藓糖醇。将不同浓度(2,3,4和6μM)的交沙霉素加入到初始化的核糖体中以开始培养。在每个培养时间将1体积的延伸混合物加入1体积的反应混合物中,并在10秒后淬灭反应。结合率由三肽形成核糖体的比例估算[1]。
动物实验 大鼠:将氚标记的交沙霉素(200mg / kg)口服给予大鼠。通过生物测定在1小时和3小时测定血液和组织水平[2]。小鼠:将氚标记的交沙霉素(200mg / kg)口服给予小鼠。通过生物测定在1小时和3小时测定血液和组织水平[2]。
参考文献

[1]. Lovmar M, et al. Kinetics of macrolide action: the Josamycin and erythromycin cases. J Biol Chem. 2004 Dec 17;279(51):53506-15.

[2]. Osono T, et al. Pharmacokinetics of macrolides, lincosamides and streptogramins. J Antimicrob Chemother. 1985 Jul;16 Suppl A:151-66.

密度 1.2±0.1 g/cm3
沸点 877.8±65.0 °C at 760 mmHg
熔点 131.5℃
分子式 C42H69NO15
分子量 827.995
闪点 484.7±34.3 °C
精确质量 827.466736
PSA 206.05000
LogP 3.88
蒸汽压 0.0±0.6 mmHg at 25°C
折射率 1.535
分子结构

1、 摩尔折射率:212.98

2、 摩尔体积(m3/mol):684.5

3、 等张比容(90.2K):1827.6

4、 表面张力(3.0 dyne/cm):50.8

5、 极化率(0.5 10 -24cm 3):84.43

计算化学

1、疏水参数计算参考值(XlogP):2.9

2、氢键供体数量:3

3、氢键受体数量:16

4、可旋转化学键数量:14

5、互变异构体数量:2

6、拓扑分子极性表面积(T6PSA):206

7、重原子数量:58

8、表面电荷:0

9、复杂度:1390

10、同位素原子数量:0

11、确定原子立构中心数量:16

12、不确定原子立构中心数量:0

13、确定化学键立构中心数量:2

14、不确定化学键立构中心数量:0

15、共价键单元数量:1

更多

1.性状:未确定

2.密度(g/mL,25/4℃):1.133g/mLat 25°C(lit.)
3.相对蒸汽密度(g/mL,空气=1):未确定

4.熔点(ºC):未确定

5.沸点(ºC,常压):151-152°C762mm Hg(lit.)

6.沸点(ºC,5.2kPa):未确定

7.折射率:n 20/D 1.528(lit.)
8.闪点(ºC):110°F
9.比旋光度(º):未确定

10.自燃点或引燃温度(ºC):未确定

11.蒸气压(kPa,25ºC):未确定

12.饱和蒸气压(kPa,60ºC):未确定

13.燃烧热(KJ/mol):未确定

14.临界温度(ºC):未确定

15.临界压力(KPa):未确定

16.油水(辛醇/水)分配系数的对数值:未确定

17.爆炸上限(%,V/V):未确定

18.爆炸下限(%,V/V):未确定

19.溶解性:未确定

毒理学数据:

急性毒性:小鼠口经LD50:>7gm/kg;大鼠LD50:6400mg/kg

CHEMICAL IDENTIFICATION

RTECS NUMBER :
OH4725810
CHEMICAL NAME :
Leucomycin V, 3-acetate 4(sup B)-(3-methylbutanoate)
CAS REGISTRY NUMBER :
16846-24-5
LAST UPDATED :
199603
DATA ITEMS CITED :
13
MOLECULAR FORMULA :
C42-H69-N-O15
MOLECULAR WEIGHT :
828.12
WISWESSER LINE NOTATION :
T-16-OV KU MUTJ DOV1 EO1 G1VH I1 JQ P1 FO- BT6OTJ CQ DN1&1 F1 EO- FT6OTJ B1 COV1Y1&1 DQ D1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
>7 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,364,1982
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
>3 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,364,1982
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
>3 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,364,1982
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
390 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
NIPDAD Nihon Daigaku No-juigakubu Gakujutsu Kenkyu Hokoku. Research Reports of the College of Agriculture and Veterinary Medicine, Nihon University. (Nihon Daigaku Nojuigakkai, 34-1 Shimouma, 3-chome, Setagaya-ku, Tokyo 154, Japan) No.1- 1953- Volume(issue)/page/year: (35),41,1978
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
6400 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 37,1565,1984
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
780 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
85GDA2 "CRC Handbook of Antibiotic Compounds," Vols.1- , Berdy, J., Boca Raton, FL, CRC Press, 1980- Volume(issue)/page/year: 2,85,1980
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
>3 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,364,1982
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
385 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
NIPDAD Nihon Daigaku No-juigakubu Gakujutsu Kenkyu Hokoku. Research Reports of the College of Agriculture and Veterinary Medicine, Nihon University. (Nihon Daigaku Nojuigakkai, 34-1 Shimouma, 3-chome, Setagaya-ku, Tokyo 154, Japan) No.1- 1953- Volume(issue)/page/year: (35),41,1978
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Mammal - species unspecified
DOSE/DURATION :
520 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
HINAAU Hindustan Antibiotics Bulletin. (Hindustan Antibiotics, Ltd., Pimpri, Poona, India) V.1- 1958- Volume(issue)/page/year: 11,26,1969
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Mammal - species unspecified
DOSE/DURATION :
786 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
HINAAU Hindustan Antibiotics Bulletin. (Hindustan Antibiotics, Ltd., Pimpri, Poona, India) V.1- 1958- Volume(issue)/page/year: 11,26,1969
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Mammal - species unspecified
DOSE/DURATION :
385 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
HINAAU Hindustan Antibiotics Bulletin. (Hindustan Antibiotics, Ltd., Pimpri, Poona, India) V.1- 1958- Volume(issue)/page/year: 11,26,1969 ** OTHER MULTIPLE DOSE TOXICITY DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
9 gm/kg/5W-I
TOXIC EFFECTS :
Liver - changes in liver weight Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases
REFERENCE :
JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 22,219,1969 ** REPRODUCTIVE DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
21 gm/kg
SEX/DURATION :
female 7-13 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Effects on Embryo or Fetus - fetal death
REFERENCE :
JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 22,219,1969

个人防护装备 Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter
危险品运输编码 NONH for all modes of transport
WGK德国 2
RTECS号 OH4725810