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硫酸奎宁

硫酸奎宁用途

硫酸奎宁(2:1)(奎拉喹)是一种从金鸡纳树皮中提取的口服活性生物碱,可用于抗疟疾研究。硫酸奎宁(2:1)是一种钾通道抑制剂,可抑制WT小鼠Slo3(KCa5.1)通道电流,该电流由+100的电压脉冲引起 mV,IC50为169μM[1][2]。
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硫酸奎宁名称

[ CAS 号 ]:
804-63-7

[ 中文名 ]:
硫酸奎宁

[ 英文名 ]:
Quinine sulfate

[英文别名 ]:

硫酸奎宁生物活性

[ 描述 ]:

硫酸奎宁(2:1)(奎拉喹)是一种从金鸡纳树皮中提取的口服活性生物碱,可用于抗疟疾研究。硫酸奎宁(2:1)是一种钾通道抑制剂,可抑制WT小鼠Slo3(KCa5.1)通道电流,该电流由+100的电压脉冲引起 mV,IC50为169μM[1][2]。

[ 相关类别 ]:

研究领域 >> 感染
信号通路 >> 跨膜转运 >> 钾通道

[体外研究]

硫酸奎宁(150μM,30分钟)抑制人肝癌HepG2细胞系中登革热病毒的增殖和细胞抑制作用[1]。硫酸奎宁(37.5-150μM,24小时)以剂量依赖性方式显著降低人肝癌HepG2细胞系中的病毒DENV RNA和蛋白质水平[1]。细胞增殖试验[1]细胞系:人肝癌细胞系(HepG2)浓度:150μM孵育时间:30分钟结果:与未处理相比,抑制DENV病毒复制,产率为19%。以剂量依赖性方式将DENV阳性细胞从23.28%减少到12.05%。

[体内研究]

硫酸奎宁(口服灌胃,12或15 mg/kg,每周,16周)对瑞士白化小鼠的皮肤癌有一定的抑制作用[2]。硫酸奎宁(口服,10 mg/kg,每日,8周)导致雄性成年白化大鼠睾丸组织抗氧化防御系统(如SOD、CAT和GSH酶活性)降低[3]。动物模型:7-8周(体重24g)的瑞士白化小鼠[2]剂量:12mg/kg,15mg/kg给药:口服灌胃;每周;16周结果:在12mg/kg剂量下,肿瘤大小和重量显著减少,而在15mg/kg更高剂量下,影响很小。

[参考文献]

[1]. Shilu Malakar,et al. Drug repurposing of quinine as antiviral against dengue virus infection. Virus Res. 2018 Aug 15;255:171-178. doi: 10.1016/j.virusres.2018.07.018. Epub 2018 Jul 25.

[2]. Jhanwar, Deepika,et al. Chemoprevention of DMBA induced skin carcinogenesis in swiss albino mice by quinine sulfate.(2016): 2636-2640.

[3]. Ebenezer O Farombi, et al. Quercetin protects against testicular toxicity induced by chronic administration of therapeutic dose of quinine sulfate in rats. J Basic Clin Physiol Pharmacol. 2012 Feb 27;23(1):39-44.

硫酸奎宁物理化学性质

[ 沸点 ]:
911.6ºC at 760 mmHg

[ 分子式 ]:
C20H26N2O6S

[ 分子量 ]:
422.495

[ 闪点 ]:
505.1ºC

[ 精确质量 ]:
422.151154

[ PSA ]:
128.57000

[ LogP ]:
3.53910

硫酸奎宁毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :
VA8440000
CHEMICAL NAME :
Quinine, sulfate
CAS REGISTRY NUMBER :
804-63-7
LAST UPDATED :
199701
DATA ITEMS CITED :
17
MOLECULAR FORMULA :
C20-H24-N2-O2.1/2H2-O4-S
MOLECULAR WEIGHT :
420.52
WISWESSER LINE NOTATION :
T66 BNJ HO1 EYQ- DT66 A B CNTJ A1U1 &WSQQ

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - woman
DOSE/DURATION :
45455 ug/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - visual field changes Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation) Kidney, Ureter, Bladder - renal function tests depressed
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - woman
DOSE/DURATION :
6500 ug/kg
TOXIC EFFECTS :
Behavioral - muscle weakness Kidney, Ureter, Bladder - interstitial nephritis
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - woman
DOSE/DURATION :
130 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Ear) - change in acuity Behavioral - changes in motor activity (specific assay)
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - man
DOSE/DURATION :
129 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation)
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - man
DOSE/DURATION :
27 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - visual field changes Sense Organs and Special Senses (Ear) - tinnitus Gastrointestinal - nausea or vomiting
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - woman
DOSE/DURATION :
12 mg/kg/1D-I
TOXIC EFFECTS :
Liver - hepatitis, fibrous (cirrhosis, post-necrotic scarring)
TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - woman
DOSE/DURATION :
220 mg/kg
TOXIC EFFECTS :
Cardiac - other changes Lungs, Thorax, or Respiration - acute pulmonary edema Blood - changes in spleen
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human
DOSE/DURATION :
4300 ug/kg
TOXIC EFFECTS :
Peripheral Nerve and Sensation - flaccid paralysis without anesthesia (usually neuromuscular blockage) Blood - agranulocytosis
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - woman
DOSE/DURATION :
80 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - visual field changes Sense Organs and Special Senses (Ear) - change in acuity Gastrointestinal - nausea or vomiting
TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - woman
DOSE/DURATION :
126 mg/kg/3W-I
TOXIC EFFECTS :
Cardiac - cardiomyopathy including infarction Skin and Appendages - dermatitis, allergic (after systemic exposure)
TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
800 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 :
1425 mg/kg
SEX/DURATION :
female 14 day(s) pre-mating - 21 day(s) post-birth
TOXIC EFFECTS :
Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) Reproductive - Effects on Newborn - physical

MUTATION DATA

TYPE OF TEST :
Phage inhibition capacity
TEST SYSTEM :
Bacteria - Escherichia coli
DOSE/DURATION :
100 ug/plate
REFERENCE :
CNREA8 Cancer Research. (Public Ledger Building, Suit 816, 6th & Chestnut Sts., Philadelphia, PA 19106) V.1- 1941- Volume(issue)/page/year: 43,2819,1983 *** REVIEWS *** TOXICOLOGY REVIEW PHJOAV Pharmaceutical Journal. (Pharmaceutical Soc. of Great Britain, 1 Lambeth High St., London, SE1 7JN, UK) V.131- 1933- Volume(issue)/page/year: 213,159,1974 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOHS - National Occupational Hazard Survey (1974) NOHS Hazard Code - 80205 No. of Facilities: 92 (estimated) No. of Industries: 3 No. of Occupations: 4 No. of Employees: 460 (estimated) NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - 80205 No. of Facilities: 82 (estimated) No. of Industries: 2 No. of Occupations: 3 No. of Employees: 1305 (estimated) No. of Female Employees: 678 (estimated)
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硫酸奎宁安全信息

[ 危险品运输编码 ]:
UN 1544

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

硫酸奎宁制备

【方法一】
由金鸡纳属树(chinchona succirubra)等的树皮提取所得奎宁经硫酸化而成。
【方法二】
该品系由苯草植物金鸡钠树皮中提取的生物碱。较重要的有四种、即奎宁、奎尼丁、辛可宁和辛可尼丁。它们者有抗疟作用,作以硅宁最强。金鸡纲树皮主要产于印尼、印度,我国台湾、海南岛和去南等地也有出产。取干燥的金鸡钠树皮粉碎,用消石和烧碱水溶液湿润,然后用乙醇浸泡提取。乙醇提取液加硫酸调pH至6-6.5,减压蒸发浓缩,同时回收乙醇。浓缩液经硫酸、烧碱处理,活性炭脱色,结晶得到粗品,再经精制而得成品。对干燥金鸡纲树皮计,总收率为2%。奎宁也可由化学合成。
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推荐生产厂家/供应商:

公司名:上海化源世纪贸易有限公司

区域:上海市普陀区

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