氯喹_用途_密度_熔点_氯喹CAS号【54-05-7】

Chloroquine 是一种广泛用于治疗疟疾和类风湿性关节炎的抗疟疾和抗炎剂。Chloroquine 是 autophagy 和 toll-like receptors (TLRs) 的抑制剂。Chloroquine 有效抑制 SARS-CoV-2 (COVID-19) 感染 (EC50=1.13 μM)。

[ 描述 ]:

Chloroquine 是一种广泛用于治疗疟疾和类风湿性关节炎的抗疟疾和抗炎剂。Chloroquine 是 autophagy 和 toll-like receptors (TLRs) 的抑制剂。Chloroquine 有效抑制 SARS-CoV-2 (COVID-19) 感染 (EC50=1.13 μM)。

[ 相关类别 ]:

信号通路 >> 免疫及炎症 >> Toll样受体(TLR)

研究领域 >> 癌症

信号通路 >> 抗感染 >> HIV

信号通路 >> 抗感染 >> SARS冠状病毒

信号通路 >> 自噬 >> 自噬

[ 靶点 ]

TLRs, HIV, SARS-CoV-2, Autophagy[1][2][3][4]

[体外研究]

氯喹(CHQ,20μM)抑制IL-12p70的释放,降低激活的人单核细胞源性Langerhans样细胞(MoLC)Th1的启动能力。氯喹(20μM)增强IL-1诱导的MoLC分泌IL-23,随后增加CD4+T细胞释放IL-17A的能力[1]。氯喹(25μM)抑制MDA-MB-231细胞正常氧和缺氧时MMP-9mrna的表达。氯喹对MMP-2、MMP-9和MMP-13mrna表达具有细胞、剂量和缺氧依赖性[2]。使用IRS-954或氯喹抑制TLR7和TLR9可显著降低HuH7细胞体外增殖[3]。氯喹(0.01-100μM；48 h)在低微极浓度(EC50=1.13 μM)下能有效阻断病毒感染(SARS-CoV-2感染vero E6细胞)。氯喹通过提高病毒/细胞融合所需的内体pH值,以及干扰SARS-CoV细胞受体的糖基化来阻断病毒感染[4]。

[体内研究]

氯喹(80mg/kg,i.p.)不能阻止原位小鼠模型中具有高或低TLR9表达水平的三阴性MDA-MB-231细胞的生长[2]。用IRS-954或氯喹抑制TLR7和TLR9可显著抑制小鼠异种移植瘤的生长。氯喹也显著抑制DEN/NMOR大鼠模型中的HCC发展[3]。

[参考文献]

[1]. Said A, et al. Chloroquine promotes IL-17 production by CD4+ T cells via p38-dependent IL-23 release by monocyte-derived Langerhans-like cells. J Immunol. 2014 Dec 15;193(12):6135-43.

[2]. Tuomela J, et al. Chloroquine has tumor-inhibitory and tumor-promoting effects in triple-negative breast cancer. Oncol Lett. 2013 Dec;6(6):1665-1672.

[3]. Mohamed FE, et al. Effect of toll-like receptor 7 and 9 targeted therapy to prevent the development of hepatocellular carcinoma. Liver Int. 2014 Jul 2. doi: 10.1111/liv.12626.

[4]. Colson P, et al. Chloroquine and hydroxychloroquine as available weapons to fight COVID-19. Int J Antimicrob Agents. 2020;55(4):105932.

[ 密度 ]:
1.1±0.1 g/cm3

[ 沸点 ]:
460.6±40.0 °C at 760 mmHg

[ 熔点 ]:
87ºC

[ 分子式 ]:
C₁₈H₂₆ClN₃

[ 分子量 ]:
319.872

[ 闪点 ]:
232.3±27.3 °C

[ 精确质量 ]:
319.181519

[ PSA ]:
28.16000

[ LogP ]:
4.69

[ 外观性状 ]:
白色粉末

[ 蒸汽压 ]:
0.0±1.1 mmHg at 25°C

[ 折射率 ]:
1.592

[ 储存条件 ]:
0-10°C;存放于惰性气体之中;避免空气,加热

CHEMICAL IDENTIFICATION

RTECS NUMBER :: VB2360000

CHEMICAL NAME :: Quinoline, 7-chloro-4-((4-(diethylamino)-1-methylbutyl)amino)-

CAS REGISTRY NUMBER :: 54-05-7

LAST UPDATED :: 199707

DATA ITEMS CITED :: 40

MOLECULAR FORMULA :: C18-H26-Cl-N3

MOLECULAR WEIGHT :: 319.92

WISWESSER LINE NOTATION :: T66 BNJ EMY1&3N2&2 IG

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 24 mg/kg/12D-I

TOXIC EFFECTS :: Brain and Coverings - changes in surface EEG Behavioral - hallucinations, distorted perceptions Behavioral - changes in motor activity (specific assay)

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 110 mg/kg

TOXIC EFFECTS :: Cardiac - change in rate Cardiac - other changes Gastrointestinal - nausea or vomiting

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 3600 mg/kg/3Y

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - visual field changes Gastrointestinal - other changes Nutritional and Gross Metabolic - weight loss or decreased weight gain

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 86 mg/kg

TOXIC EFFECTS :: Cardiac - change in rate Cardiac - other changes Gastrointestinal - nausea or vomiting

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human

DOSE/DURATION :: 20 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - diplopia Behavioral - coma Vascular - BP elevation not characterized in autonomic section

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - child

DOSE/DURATION :: 37593 ug/kg

TOXIC EFFECTS :: Brain and Coverings - other degenerative changes Behavioral - convulsions or effect on seizure threshold Cardiac - change in rate

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 330 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Behavioral - ataxia Lungs, Thorax, or Respiration - dyspnea

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 102 mg/kg

TOXIC EFFECTS :: Gastrointestinal - other changes

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 190 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 :: 60 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 :: 311 mg/kg

TOXIC EFFECTS :: Behavioral - tremor Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory depression

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 66 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 - mouse

DOSE/DURATION :: 150 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 :: 21600 ug/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 :: Intramuscular

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 71 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 - rabbit

DOSE/DURATION :: 75 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 - rabbit

DOSE/DURATION :: 8 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 :: Intramuscular

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 20 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

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 560 mg/kg/14D-I

TOXIC EFFECTS :: Behavioral - food intake (animal) Nutritional and Gross Metabolic - weight loss or decreased weight gain Related to Chronic Data - death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 9800 mg/kg/35W-C

TOXIC EFFECTS :: Behavioral - food intake (animal) Blood - changes in leukocyte (WBC) count Nutritional and Gross Metabolic - weight loss or decreased weight gain

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 360 mg/kg/30D-I

TOXIC EFFECTS :: Behavioral - tremor Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases Related to Chronic Data - death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Unreported

DOSE :: 420 mg/kg

SEX/DURATION :: female 1-42 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - urogenital system Reproductive - Specific Developmental Abnormalities - other developmental abnormalities

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Unreported

DOSE :: 1155 mg/kg

SEX/DURATION :: female 6-39 week(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - eye/ear Reproductive - Effects on Newborn - other postnatal measures or effects

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Unreported

DOSE :: 840 mg/kg

SEX/DURATION :: female 1-84 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - abortion

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 10500 mg/kg

SEX/DURATION :: female 1-15 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - musculoskeletal system Reproductive - Specific Developmental Abnormalities - hepatobiliary system

TYPE OF TEST :: Specific locus test

TYPE OF TEST :: Sex chromosome loss and nondisjunction

MUTATION DATA

TYPE OF TEST :: DNA damage

TEST SYSTEM :: Mammal - species unspecified Lymphocyte

DOSE/DURATION :: 500 umol/L

REFERENCE :: BBACAQ Biochimica et Biophysica Acta. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1947- Volume(issue)/page/year: 561,77,1979 *** REVIEWS *** IARC Cancer Review:Animal Inadequate Evidence IMEMDT IARC Monographs on the Evaluation of Carcinogenic Risk of Chemicals to Man. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) V.1- 1972- Volume(issue)/page/year: 13,47,1977 IARC Cancer Review:Human No Adequate Data IMEMDT IARC Monographs on the Evaluation of Carcinogenic Risk of Chemicals to Man. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) V.1- 1972- Volume(issue)/page/year: 13,47,1977 IARC Cancer Review:Group 3 IMSUDL IARC Monographs, Supplement. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) No.1- 1979- Volume(issue)/page/year: 7,56,1987 TOXICOLOGY REVIEW PLMJAP Pahlavi Medical Journal. (Shiraz, Iran) V.1-9, 1970-78. Volume(issue)/page/year: 6,160,1975 TOXICOLOGY REVIEW 32XPAD "Teratology," Berry, C.L., and D.E. Poswillo, eds., New York, Springer, 1975 Volume(issue)/page/year: -,49,1975 TOXICOLOGY REVIEW FNSCA6 Forensic Science. (Lausanne, Switzerland) V.1-11, 1972-78. For pub lisher information, see FSINDR. Volume(issue)/page/year: 2,67,1973 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X4820 No. of Facilities: 7 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 103 (estimated) No. of Female Employees: 52 (estimated)

[ 危害码 (欧洲) ]:
Xi

[ 海关编码 ]:
2933499090

详细合成路线

氯喹上游产品

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[ 海关编码 ]: 2933499090

[ 中文概述 ]:
2933499090. 其他含喹琳或异喹啉环系的化合物〔但未进一步稠合的〕. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933499090. other compounds containing in the structure a quinoline or isoquinoline ring-system (whether or not hydrogenated), not further fused. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

公司名：上海吉至生化科技有限公司

区域：上海市奉贤区

价格：
￥258.0/50mg ￥778.0/250mg

联系人：刘佳

产品详情：氯喹

公司名：上海脉铂医药科技有限公司

区域：上海市嘉定区

价格：
￥450.0/250mg ￥需询单/1g ￥需询单/1g ￥需询单/1g

联系人：李先生

产品详情：氯喹

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：
￥69.9/250mg ￥139.9/1ml ￥204.9/1g ￥3352.9/25g

联系人：阿拉丁

产品详情：氯喹

公司名：上海创赛科技有限公司

区域：上海市嘉定区

价格：
￥159.0/50mg ￥355.0/250mg ￥982.0/1g ￥2847.0/5g

联系人：夏言

产品详情：[Perfemiker]氯喹,97%

公司名：武汉敬康恩生物医药科技有限公司

区域：武汉市东西湖区

价格：
￥需询单/1g

联系人：周经理

产品详情：CHLOROQUINE

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