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564-25-0

564-25-0结构式
564-25-0结构式
  • 常用中文名:强力霉素
  • 常用英文名:Doxycycline
  • CAS号:564-25-0
  • 分子式:C22H24N2O8
  • 分子量:444.435
  • 相关类别: 原料药 抗生素类药物 四环素类药
  • 发布时间:2018-05-13 08:00:00
  • 更新时间:2024-01-02 08:06:04
  • Doxycycline 是一种四环素抗生素,口服有效的,广谱的金属蛋白酶 (MMP) 抑制剂,具有抗菌活性。

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中文名 强力霉素
英文名 doxycycline
中文别名 脱氧土霉素
6-甲基-4-(二甲氨基)-3,5,10,12,12a-五羟基-1,11-二氧代-1,4,4a,5,5a,6,11,12a-八氢-2-并四苯甲酰胺
英文别名 Monodox
azudoxat
Doxycen
MFCD02682958
gs-3065
(2Z,4S,4aR,5S,5aR,6R,12aS)-2-[amino(hydroxy)methylidene]-4-(dimethylamino)-5,10,11,12a-tetrahydroxy-6-methyl-4a,5a,6,12a-tetrahydrotetracene-1,3,12(2H,4H,5H)-trione
(2Z,4S,4aR,5S,5aR,6R,12aS)-2-[Amino(hydroxy)methylene]-4-(dimethylamino)-5,10,11,12a-tetrahydroxy-6-methyl-4a,5a,6,12a-tetrahydro-1,3,12(2H,4H,5H)-tetracenetrione
1,3,12(2H,4H,5H)-Naphthacenetrione, 2-(aminohydroxymethylene)-4-(dimethylamino)-4a,5a,6,12a-tetrahydro-5,10,11,12a-tetrahydroxy-6-methyl-, (2Z,4S,4aR,5S,5aR,6R,12aS)-
Ronaxan
doxocycline
doryx
Unidox
(2Z,4S,4aR,5S,5aR,6R,12aS)-2-[Amino(hydroxy)methylene]-4-(dimethylamino)-5,10,11,12a-tetrahydroxy-6-methyl-4a,5a,6,12a-tetrahydrotetracene-1,3,12(2H,4H,5H)-trione
doxitard
Doxycycline
spanor
Doxinyl
EINECS 209-271-1
描述 Doxycycline 是一种四环素抗生素,口服有效的,广谱的金属蛋白酶 (MMP) 抑制剂,具有抗菌活性。
相关类别
体外研究 多西环素仅在高浓度下影响胶质瘤细胞的生长[2]。多西环素降低SVG细胞中MT-CO1蛋白含量,浓度为1μg/mL或更高[2]。细胞增殖测定[2]细胞系:LNT-229、G55和U343胶质瘤细胞浓度:0.01、0.1、1或10μg/mL培养时间:4天结果:仅在高浓度下影响胶质瘤细胞的生长。Western Blot分析[2]细胞系:SVG细胞浓度:0.01,0.1,1或10μg/mL培养时间:24小时结果:浓度为1μg/mL或更高的MT-CO1蛋白含量降低。
体内研究 多西环素(口服;200或800mg/kg/天;3个月)以剂量依赖性方式降低未治疗HT小鼠中的活性MMP-9[1]。动物模型:6个月大的雌性杂合子Col3a1缺陷(HT)小鼠[1]剂量:200或800 mg/kg给药:口服;每天;持续3个月结果:活性MMP-9以剂量依赖性方式降低。
参考文献

[1]. Briest W, et al. Doxycycline ameliorates the susceptibility to aortic lesions in a mouse model for the vascular type of Ehlers-Danlos syndrome. J Pharmacol Exp Ther. 2011 Jun;337(3):621-7.

[2]. Luger AL, et al. Doxycycline Impairs Mitochondrial Function and Protects Human Glioma Cells from Hypoxia-Induced Cell Death: Implications of Using Tet-Inducible Systems. Int J Mol Sci. 2018 May 17;19(5).

密度 1.6±0.1 g/cm3
沸点 685.2±55.0 °C at 760 mmHg
熔点 206-209ºC
分子式 C22H24N2O8
分子量 444.435
闪点 368.2±31.5 °C
精确质量 444.153259
PSA 181.62000
LogP 1.36
外观性状 黄色晶体粉末
蒸汽压 0.0±2.2 mmHg at 25°C
折射率 1.737
储存条件 2-8C

CHEMICAL IDENTIFICATION

RTECS NUMBER :
QI8650000
CHEMICAL NAME :
2-Naphthacenecarboxamide, 4-alpha-S-(dimethylamino)-1,4,4a-alpha-5,5a-alpha,6,1 1,12a- octahydro-3,5-alpha,10,12,12a-alpha-pentahydroxy-6-al pha-methyl-1,11-dioxo-
CAS REGISTRY NUMBER :
564-25-0
LAST UPDATED :
199609
DATA ITEMS CITED :
15
MOLECULAR FORMULA :
C22-H24-N2-O8
MOLECULAR WEIGHT :
444.48
WISWESSER LINE NOTATION :
L E6 C666 BV FV CU GUTTT&J DQ GVZ HQ IN1&1 KQ MQ M1 RQ

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - woman
DOSE/DURATION :
68 mg/kg/24D-I
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
>2 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
378 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
228 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
1870 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
410 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
241 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
>500 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
>100 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
750 mg/kg
SEX/DURATION :
female 2 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)

MUTATION DATA

TYPE OF TEST :
DNA inhibition
TEST SYSTEM :
Human Lymphocyte
DOSE/DURATION :
3750 ug/L
REFERENCE :
BCPHBM British Journal of Clinical Pharmacology. (Blackwell Scientific Pub. Ltd., POB 88, Oxford, UK) V.1- 1974- Volume(issue)/page/year: 16,127,1983 *** REVIEWS *** TOXICOLOGY REVIEW PBPSDY Pharmacological and Biochemical Properties of Drug Substances. (American Pharmaceutical Assoc., 2215 Constitution Ave., NW, Washington, DC 20037) V.1- 1977- Volume(issue)/page/year: 2,305,1979 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOHS - National Occupational Hazard Survey (1974) NOHS Hazard Code - 84744 No. of Facilities: 641 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 1281 (estimated) NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - 84744 No. of Facilities: 450 (estimated) No. of Industries: 1 No. of Occupations: 5 No. of Employees: 22055 (estimated) No. of Female Employees: 18813 (estimated)

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