18323-44-9

• 常用中文名：克林霉素
• 常用英文名：Clindamycin
• CAS号：18323-44-9
• 分子式：C₁₈H₃₃ClN₂O₅S
• 分子量：424.983
• 相关类别： 原料药 抗生素类药物 林可胺类药
• 发布时间：2018-06-19 10:39:06
• 更新时间：2024-01-02 07:23:10
• Clindamycin 是一种口服有效的蛋白质合成抑制剂,其具有以亚抑制浓度 (sub-MICs) 在金黄色葡萄球菌中毒力因子表达的能力。Clindamycin 的抗性是由 50S 核糖体亚基 (23S rRNA) 中抗生素结合位点的酶促甲基化产生。Clindamycin 降低杀白细胞毒素 (PVL),毒性休克-葡萄球菌毒素 (TSST-1) 或 α-溶血素 (Hla) 的产生。

名称

• 中文名: 氯洁霉素
• 英文名: clindamycin
• 中文别名: 克林霉素; 氯林霉素
• 英文别名: L-threo-α-D-galacto-Octopyranoside, methyl 7-chloro-6,7,8-trideoxy-6-[[[(2S,4R)-1-methyl-4-propyl-2-pyrrolidinyl]carbonyl]amino]-1-thio-; 7-Deoxy-7(S)-chlorolincomycin; EINECS 242-209-1; Chlorodeoxylincomycin; Methyl 7-Chloro-6,7,8-trideoxy-6-[[[(2S,4R)-1-methyl-4-propyl-2-pyrrolidinyl]carbonyl]amino]-1-thio-L-threo-a-D-galacto-octopyranoside; Cleocin; Clindamycin; Methyl (2S-trans)-7-Chloro-6,7,8-trideoxy-6-[[(1-methyl-4-propyl-2-pyrrolidinyl)carbonyl]amino]-1-thio-L-threo-a-D-galacto-octopyranoside; 7-CDL; L-threo-α-D-galacto-Octopyranoside, methyl 7-chloro-6,7,8-trideoxy-6-((((2S,4R)-1-methyl-4-propyl-2-pyrrolidinyl)carbonyl)amino)-1-thio-; MFCD00072005; (2S,4R)-N-{(1S,2S)-2-Chlor-1-[(2R,3R,4S,5R,6R)-3,4,5-trihydroxy-6-(methylsulfanyl)tetrahydro-2H-pyran-2-yl]propyl}-1-methyl-4-propylpyrrolidin-2-carboxamid; CLDM; Methyl 7-chloro-6,7,8-trideoxy-6-{[(4R)-1-methyl-4-propyl-L-prolyl]amino}-1-thio-L-threo-α-D-galacto-octopyranoside; dalacinc; Dalacine; clinimycin; Methyl (5R)-5-[(1S,2S)-2-chloro-1-{[(4R)-1-methyl-4-propyl-L-prolyl]amino}propyl]-1-thio-β-L-arabinopyranoside; 7-Chlorolincomycin; sobelin; (2S,4R)-N-{(1S,2S)-2-chloro-1-[(2R,3R,4S,5R,6R)-3,4,5-trihydroxy-6-(methylsulfanyl)tetrahydro-2H-pyran-2-yl]propyl}-1-methyl-4-propylpyrrolidine-2-carboxamide; (2S,4R)-N-{(1S,2S)-2-chloro-1-[(2R,3R,4S,5R,6R)-3,4,5-trihydroxy-6-(méthylsulfanyl)tétrahydro-2H-pyran-2-yl]propyl}-1-méthyl-4-propylpyrrolidine-2-carboxamide; chlolincocin

物化性质

• 密度: 1.3±0.1 g/cm3
• 沸点: 628.1±55.0 °C at 760 mmHg
• 熔点: 141 - 143ºC
• 分子式: C₁₈H₃₃ClN₂O₅S
• 分子量: 424.983
• 闪点: 333.6±31.5 °C
• 精确质量: 424.179871
• PSA: 127.56000
• LogP: 1.83
• 外观性状: 白色结晶粉末
• 蒸汽压: 0.0±4.2 mmHg at 25°C
• 折射率: 1.574
• 储存条件: -20℃

生物活性

• 描述: Clindamycin 是一种口服有效的蛋白质合成抑制剂,其具有以亚抑制浓度 (sub-MICs) 在金黄色葡萄球菌中毒力因子表达的能力。Clindamycin 的抗性是由 50S 核糖体亚基 (23S rRNA) 中抗生素结合位点的酶促甲基化产生。Clindamycin 降低杀白细胞毒素 (PVL),毒性休克-葡萄球菌毒素 (TSST-1) 或 α-溶血素 (Hla) 的产生。
• 相关类别:
  研究领域 >> 感染
  信号通路 >> 抗感染 >> 细菌
• 参考文献:

  [1]. Hodille E, et al. Clindamycin suppresses virulence expression in inducible clindamycin-resistant Staphylococcus aureus strains. Ann Clin Microbiol Antimicrob. 2018 Oct 20;17(1):38.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : RH6300000 CHEMICAL NAME : L-threo-D-galacto-Octopyranoside, methyl 7-chloro-6,7,8-trideoxy-6-(1-methyl-4-propyl-L-2- pyrrolidinecarboxamido)-1-thio-, trans-alpha- CAS REGISTRY NUMBER : 18323-44-9 LAST UPDATED : 199606 DATA ITEMS CITED : 5 MOLECULAR FORMULA : C18-H33-Cl-N2-O5-S MOLECULAR WEIGHT : 425.04 WISWESSER LINE NOTATION : T6OTJ BS1 CQ DQ EQ FYYG1&MV- BT5NTJ A1 D3 HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 2618 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 18,185,1971 TYPE OF TEST : LDLo - Lowest published lethal dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rabbit DOSE/DURATION : 1 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : RMVEAG Recueil de Medecine Veterinaire. (Masson Pub. USA, Inc., Year Book Medical Pub., 35 E. Wacker Dr., Chicago IL 60601) V.1- 1824- Volume(issue)/page/year: 156,915,1980 TYPE OF TEST : LDLo - Lowest published lethal dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - hamster DOSE/DURATION : 1 mg/kg TOXIC EFFECTS : Gastrointestinal - other changes REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 34,794,1984 ** OTHER MULTIPLE DOSE TOXICITY DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rabbit DOSE/DURATION : 330 mg/kg/33D-I TOXIC EFFECTS : Gastrointestinal - other changes REFERENCE : ANTBAL Antibiotiki. (Moscow, USSR) V.1-29, 1956-84. For publisher information, see AMBIEH. Volume(issue)/page/year: 28,18,1983 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X3191 No. of Facilities: 445 (estimated) No. of Industries: 1 No. of Occupations: 7 No. of Employees: 21575 (estimated) No. of Female Employees: 17442 (estimated)