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磷酸氯喹

磷酸氯喹用途

Chloroquine diphosphate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药。 Chloroquine 是 autophagy 和 toll-like receptors (TLRs) 的抑制剂。

磷酸氯喹名称

[ CAS 号 ]:
50-63-5

[ 中文名 ]:
磷酸氯喹

[ 英文名 ]:
Chloroquine diphosphate

[中文别名 ]:

[英文别名 ]:

MFCD00069852
Chloroquine phosphate
EINECS 200-055-2
Chloroquine diphosphate salt
Aralen phosphate
Chloroquine diphosphate
Imagon
Tresochin
Chloroquinediphosphate
Malaquin

磷酸氯喹生物活性

[ 描述 ]:

Chloroquine diphosphate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药。 Chloroquine 是 autophagy 和 toll-like receptors (TLRs) 的抑制剂。

[ 相关类别 ]:

信号通路 >> 自噬 >> 自噬

信号通路 >> 免疫及炎症 >> Toll样受体(TLR)

研究领域 >> 炎症/免疫

[ 靶点 ]

Autophagy, TLRs[1][2][3]

[体外研究]

氯喹(CHQ,20μM)抑制IL-12p70释放并降低活化的人单核细胞衍生的朗格汉斯样细胞(MoLC)的Th1引发能力。氯喹(CHQ,20μM)增强MoLC中IL-1诱导的IL-23分泌,随后通过引发的CD4 + T细胞增加IL-17A释放[1]。氯喹(25μM)抑制亲本MDA-MB-231细胞中常氧和缺氧中的MMP-9mRNA表达。氯喹对MMP-2,MMP-9和MMP-13 mRNA表达具有细胞,剂量和缺氧依赖性作用[2]。使用IRS-954或氯喹抑制TLR7和TLR9可显着降低体外HuH7细胞的增殖[3]。

[体内研究]

氯喹(80 mg/kg,ip)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]。使用IRS-954或氯喹的TLR7和TLR9抑制显着抑制小鼠异种移植模型中的肿瘤生长。 DEN/NMOR大鼠模型中的HCC发育也被氯喹显着抑制[3]。

[细胞实验]

将细胞在载体或25或50μM氯喹存在下在具有正常培养基的6孔板中培养，直至接近汇合，之后用无菌磷酸盐缓冲盐水（PBS）冲洗并进一步培养指定的时间。在无血清培养基中。在所需的时间点，弃去培养基并在裂解缓冲液中快速收获细胞并通过离心澄清。在还原十二烷基硫酸钠（SDS）样品缓冲液中煮沸上清液后，每道加载等量的蛋白质（100μg），将样品电泳到10或4-20％梯度聚丙烯酰胺SDS凝胶中，然后转移到硝酸纤维素膜上。膜。为了检测TLR9，将印迹在4℃下与抗TLR9抗体一起温育过夜，在含有0.1％（v / v）Tween-20（TBST）的Tris缓冲盐水中1：500稀释。用多克隆兔抗肌动蛋白确认等量加载。用辣根过氧化物酶连接的二抗进行二次检测。使用ECL试剂盒通过化学发光使蛋白质条带可视化。

[动物实验]

将对照和TLR9 siRNA MDA-MB-231细胞（100μL中的5×10 5个细胞）接种到4周龄免疫缺陷小鼠（无胸腺裸/ nu Foxn1）的乳房脂肪垫中。在肿瘤细胞接种后7天开始治疗。每天用腹膜内（ip）氯喹（80mg / kg）或载体（PBS）处理小鼠。每天监测动物的临床症状。每周进行两次肿瘤测量，并根据公式V =（π/ 6）（d1×d2）3/2计算肿瘤体积，其中d1和d2是垂直肿瘤直径。使肿瘤生长22天，此时处死小鼠并解剖肿瘤用于最终测量。在整个实验中，将动物维持在受控制的无病原体环境条件下（20-21℃，30-60％相对湿度和12小时光照循环）。给小鼠喂食小动物食物颗粒，随意提供无菌水。

[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.

[相关活性小分子]

磷酸氯喹物理化学性质

[ 沸点 ]:
460.6ºC at 760 mmHg

[ 熔点 ]:
200 °C (dec.)(lit.)

[ 分子式 ]:
C₁₈H₃₂ClN₃O₈P₂

[ 分子量 ]:
515.862

[ 闪点 ]:
232.3ºC

[ 精确质量 ]:
515.135315

[ PSA ]:
203.30000

[ LogP ]:
3.02640

[ 外观性状 ]:
白色固体

[ 储存条件 ]:
Desiccate at RT

[ 水溶解性 ]:
H2O: 50 mg/mL, clear

磷酸氯喹MSDS

详细MSDS(安全技术说明书)

磷酸氯喹毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: VB2450000

CHEMICAL NAME :: Quinoline, 7-chloro-4-(4-diethylamino-1-methyl-butylamino)-, diphosphate

CAS REGISTRY NUMBER :: 50-63-5

LAST UPDATED :: 199606

DATA ITEMS CITED :: 30

MOLECULAR FORMULA :: C18-H26-Cl-N3.2H3-O4-P

MOLECULAR WEIGHT :: 515.92

WISWESSER LINE NOTATION :: T66 BNJ EMY1&3N2&2 IG &P2-O6

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 8571 ug/kg

TOXIC EFFECTS :: Gastrointestinal - nausea or vomiting Gastrointestinal - other changes

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 8571 ug/kg

TOXIC EFFECTS :: Gastrointestinal - ulceration or bleeding from duodenum Gastrointestinal - nausea or vomiting Gastrointestinal - other changes

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - child

DOSE/DURATION :: 250 mg/kg

TOXIC EFFECTS :: Behavioral - coma

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 167 mg/kg

TOXIC EFFECTS :: Cardiac - EKG changes not diagnostic of specified effects Vascular - BP lowering not characterized in autonomic section Lungs, Thorax, or Respiration - respiratory depression

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 179 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 :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 600 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 :: 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 :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 68 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 200 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 :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 8 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity)

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Bird - domestic

DOSE/DURATION :: 64500 ug/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 :: 8820 mg/kg/21W-C

TOXIC EFFECTS :: Cardiac - other changes Liver - hepatitis (hepatocellular necrosis), diffuse Related to Chronic Data - death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 840 mg/kg/21D-I

TOXIC EFFECTS :: Behavioral - food intake (animal) Kidney, Ureter, Bladder - urine volume decreased Nutritional and Gross Metabolic - weight loss or decreased weight gain

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 400 mg/kg/10D-I

TOXIC EFFECTS :: Kidney, Ureter, Bladder - proteinuria Kidney, Ureter, Bladder - other changes in urine composition Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - phosphatases

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Ocular

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 72 ug/kg/12D-I

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - corneal damage

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 280 mg/kg/14D-I

TOXIC EFFECTS :: Behavioral - tremor Related to Chronic Data - death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Primate - monkey

DOSE/DURATION :: 1 gm/kg/10D-I

TOXIC EFFECTS :: Liver - fatty liver degeneration 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

DOSE :: 1200 mg/kg

SEX/DURATION :: female 5-16 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 550 mg/kg

SEX/DURATION :: female 9 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - eye/ear

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 750 mg/kg

SEX/DURATION :: female 9 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetal death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 80 mg/kg

SEX/DURATION :: female 20-21 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - respiratory system Reproductive - Effects on Newborn - physical

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 475 mg/kg

SEX/DURATION :: female 10-14 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Newborn - physical

MUTATION DATA

TYPE OF TEST :: Sister chromatid exchange

TEST SYSTEM :: Rodent - hamster Lung

DOSE/DURATION :: 100 ug/L

REFERENCE :: CBTOE2 Cell Biology and Toxicology. (Princeton Scientific Pub., Inc., 301 N. Harrison St., CN 5279, Princeton, NJ 08540) V.1- 1984- Volume(issue)/page/year: 2,379,1986 *** REVIEWS *** TOXICOLOGY REVIEW INTEAG Internist. (Springer-Verlag New York, Inc., Service Center, 44 Hartz Way, Secaucus, NJ 07094) V.1- 1960- Volume(issue)/page/year: 15,7,1974 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X4486 No. of Facilities: 40 (estimated) No. of Industries: 2 No. of Occupations: 3 No. of Employees: 644 (estimated) No. of Female Employees: 238 (estimated)

磷酸氯喹安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

[ 警示性声明 ]:
P301 + P312 + P330

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xn:Harmful;

[ 风险声明 (欧洲) ]:
R22

[ 安全声明 (欧洲) ]:
S22-S24/25

[ 危险品运输编码 ]:
1544

[ WGK德国 ]:
3

[ RTECS号 ]:
VB2450000

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

[ 海关编码 ]:
2933499090

磷酸氯喹上下游产品

磷酸氯喹上游产品

磷酸氯喹下游产品

磷酸氯喹制备

4,7-二氯喹啉与2-氨基-5二乙氨基戊烷缩合，得到氯喹。

磷酸氯喹海关

[ 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%

磷酸氯喹文献

Itraconazole suppresses the growth of glioblastoma through induction of autophagy: involvement of abnormal cholesterol trafficking.

Autophagy 10(7) , 1241-55, (2014)

Glioblastoma is one of the most aggressive human cancers with poor prognosis, and therefore a critical need exists for novel therapeutic strategies for management of glioblastoma patients. Itraconazol...

Regulators of autophagosome formation in Drosophila muscles.

PLoS Genet. 11(2) , e1005006, (2015)

Given the diversity of autophagy targets and regulation, it is important to characterize autophagy in various cell types and conditions. We used a primary myocyte cell culture system to assay the role...

An integrated biological approach to guide the development of metal-chelating inhibitors of influenza virus PA endonuclease.

Mol. Pharmacol. 87(2) , 323-37, (2015)

The influenza virus PA endonuclease, which cleaves capped cellular pre-mRNAs to prime viral mRNA synthesis, is a promising target for novel anti-influenza virus therapeutics. The catalytic center of t...

更多文献

磷酸氯喹相关知识

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2020-02-18 21:54:03

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