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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 ]:

[ 相关类别 ]:

研究领域 >> 癌症

研究领域 >> 感染

研究领域 >> 炎症/免疫

信号通路 >> 抗感染 >> 细菌

[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]

[1]. I Chopra, et al. Tetracyclines, molecular and clinical aspects. J Antimicrob Chemother. 1992 Mar;29(3):245-77.

[2]. D Schnappinger, et al. Tetracyclines: antibiotic action, uptake, and resistance mechanisms. Arch Microbiol. 1996 Jun;165(6):359-69.

[3]. Marleen L A Kortenoeven, et al. Demeclocycline attenuates hyponatremia by reducing aquaporin-2 expression in the renal inner medulla. Am J Physiol Renal Physiol. 2013 Dec 15;305(12):F1705-18.

[4]. Susobhan Sarkar, et al. Demeclocycline Reduces the Growth of Human Brain Tumor-Initiating Cells: Direct Activity and Through Monocytes. Front Immunol. 2020 Feb 21;11:272.

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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地美环素

地美环素用途

地美环素名称

地美环素生物活性

地美环素物理化学性质

地美环素毒性和生态

CHEMICAL IDENTIFICATION

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

MUTATION DATA

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