地美环素
地美环素用途
去甲环素是一种口服活性四环素抗生素。去甲环素通过与30S核糖体亚基结合来抑制氨基酰基tRNA的结合,从而损害蛋白质合成。脱氯环素对多种细菌感染具有抗菌活性[1][2]。
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地美环素名称
[ CAS 号 ]:
127-33-3
[ 中文名 ]:
地美环素
[ 英文名 ]:
Demeclocycline
[英文别名 ]:
- Ledermycin hydrochloride
- 7-chloro-6-demethyltetracycline
- 6-demethyl-7-chlorotetracycline
- Elkamicina
- DMCTC
- Declomycin
- EINECS 204-834-8
- Demeclocyclinum
- Demethylchlortetracycline(DMCT)
- Demeclociclina
地美环素生物活性
[ 描述 ]:
去甲环素是一种口服活性四环素抗生素。去甲环素通过与30S核糖体亚基结合来抑制氨基酰基tRNA的结合,从而损害蛋白质合成。脱氯环素对多种细菌感染具有抗菌活性[1][2]。
[ 相关类别 ]:
[体外研究]
脱氯环素(0-100μM；24小时)处理降低mpkCCD细胞中AQP2的丰度[3]。去甲环素(10μM；24小时)治疗促进单核细胞和巨噬细胞的活性[4]。去甲环素(1-10μM；72小时)治疗直接影响脑肿瘤细胞的生长[4]。Western印迹分析[3]细胞系：MpkCCD细胞浓度：0-100μM孵育时间：24小时结果：MpkCCD细胞中AQP2丰度降低,在50μM时有显著影响。细胞存活率测定[4]细胞系：小鼠骨髓来源的巨噬细胞和单核细胞浓度：10μM孵育时间：24小时结果：增强TNF-α的产生并调节单核细胞功能。细胞存活率测定[4]细胞系：脑肿瘤起始细胞浓度：1、5和10μM孵育时间：72小时结果：通过两种方式抑制细胞生长：使用单核细胞作为中介,并直接影响脑肿瘤起始的细胞增殖和球体形成能力。
[体内研究]
去甲环素(腹腔注射；40mg/kg；每日一次；48小时)治疗可显著降低低钠血症,显著纠正低渗透压,且无肾毒性[3]。动物模型：低钠血症雄性Wistar大鼠[3]剂量：40mg/kg给药：腹腔注射；40mg/kg；每日一次；48小时结果：尿量增加,尿渗透压降低,并导致水排泄分数显著增加。动物模型：低钠血症雄性Wistar大鼠[3]剂量：40mg/kg给药：腹腔注射；40mg/kg；每日一次；48小时结果：表明肾内髓质对AQP2和AC5/6有特异性作用,而非二次毒性作用。
[参考文献]
地美环素物理化学性质
[ 密度 ]:
1.8±0.1 g/cm3
[ 沸点 ]:
684.5±55.0 °C at 760 mmHg
[ 分子式 ]:
C21H21ClN2O8
[ 分子量 ]:
464.853
[ 闪点 ]:
367.8±31.5 °C
[ 精确质量 ]:
464.098633
[ PSA ]:
181.62000
[ LogP ]:
0.57
[ 蒸汽压 ]:
0.0±2.2 mmHg at 25°C
[ 折射率 ]:
1.761
[ 储存条件 ]:
室温
地美环素毒性和生态
CHEMICAL IDENTIFICATION
- RTECS NUMBER :
- QI7650000
- CHEMICAL NAME :
- 2-Naphthacenecarboxamide, 7-chloro-4-(dimethylamino)-1,4,4a,5,5a,6,11,12a-octah ydro- 3,6,10,12,12a-pentahydroxy-1,11-dioxo-
- CAS REGISTRY NUMBER :
- 127-33-3
- LAST UPDATED :
- 199706
- DATA ITEMS CITED :
- 15
- MOLECULAR FORMULA :
- C21-H21-Cl-N2-O8
- MOLECULAR WEIGHT :
- 464.89
- WISWESSER LINE NOTATION :
- L E6 C666 BV FV CU GUTTT&J DQ EQ GVZ HQ IN1&1 MQ OG RQ
HEALTH HAZARD DATA
ACUTE TOXICITY DATA
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Human
- DOSE/DURATION :
- 420 mg/kg/6W
- TOXIC EFFECTS :
- Endocrine - diabetes insipidus (nephrogenic or CNS) Biochemical - Metabolism (Intermediary) - effect on cyclic nucleotides
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Human
- DOSE/DURATION :
- 10 mg/kg
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Human
- DOSE/DURATION :
- 68 mg/kg/8D
- TOXIC EFFECTS :
- Kidney, Ureter, Bladder - urine volume increased Kidney, Ureter, Bladder - other changes in urine composition
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- >6750 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 - rat
- DOSE/DURATION :
- 358 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 :
- Subcutaneous
- 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 :
- LDLo - Lowest published lethal dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 4 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 - mouse
- DOSE/DURATION :
- 454 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- TYPE OF TEST :
- LDLo - Lowest published lethal dose
- ROUTE OF EXPOSURE :
- Subcutaneous
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 2500 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 :
- 79 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 :
- Unreported
- DOSE :
- 240 mg/kg
- SEX/DURATION :
- female 1-39 week(s) after conception
- TOXIC EFFECTS :
- Reproductive - Effects on Newborn - other postnatal measures or effects
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- DOSE :
- 5 gm/kg
- SEX/DURATION :
- female 1-22 day(s) after conception lactating female 21 day(s) post-birth
- TOXIC EFFECTS :
- Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue) Reproductive - Specific Developmental Abnormalities - skin and skin appendages Reproductive - Effects on Newborn - weaning or lactation index (e.g., # alive at weaning per # alive at day 4)
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- DOSE :
- 5 gm/kg
- SEX/DURATION :
- female 1-22 day(s) after conception lactating female 21 day(s) post-birth
- TOXIC EFFECTS :
- Reproductive - Effects on Newborn - other postnatal measures or effects
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 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X5539 No. of Facilities: 10 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 330 (estimated) No. of Female Employees: 120 (estimated)
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推荐生产厂家/供应商：
公司名：上海源溪生物科技有限公司
区域：上海市浦东新区
价格：
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联系人：赖经理
产品详情：Declostatin
公司名：上海阿拉丁生化科技股份有限公司
区域：上海市浦东新区
价格：
￥758.0/5mg
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相关化合物
【地美环素】化源网提供地美环素CAS号127-33-3，地美环素MSDS及其说明、性质、英文名、生产厂家、作用/用途、分子量、密度、沸点、熔点、结构式等。CAS号查询地美环素上化源网，专业又轻松。>>电脑版：地美环素
标题：地美环素_用途_密度_沸点_地美环素CAS号【127-33-3】_化源网 地址：https://m.chemsrc.com/mip/cas/127-33-3_511296.html