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海恩酮

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Hycanthone 是一种有效的抗血吸虫药物。

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海恩酮名称

[ CAS 号 ]:
3105-97-3

[ 中文名 ]:
海恩酮

[ 英文名 ]:
Hycanthone

[中文别名 ]:

[英文别名 ]:

lucanthonemetabolite
ETRENOL
hycanthon
Win 249-33
Etrenol(mesylate)
HYCANTHONE

海恩酮生物活性

[ 描述 ]:

Hycanthone 是一种有效的抗血吸虫药物。

[ 相关类别 ]:

信号通路 >> 抗感染 >> 寄生物

研究领域 >> 感染

[ 靶点 ]

Parasite[1]

[体外研究]

20mg/mL或更高的Hycanthone对细胞活力逐渐更不利。结果显示,与对照相比,Hycanthone浓度增加0.1至10μg/ mL,可使病毒干扰素产量逐渐降低73％[2]。

[体内研究]

结果表明,用Hycanthone处理后,氚标记的胸苷掺入成虫敏感性蠕虫的TCA可沉淀物质中逐渐减少。在任何时候测试,未成熟的蠕虫完全不受Hycanthone的影响。用Hycanthone处理的雄性蠕虫表现出从最初的低水平掺入可能部分恢复的迹象。用Hycanthone处理的药物敏感性蠕虫掺入氚化亮氨酸在处理后的前四天被抑制40％至50％。结果显示,在Hycanthone处理后7天,两种核糖体RNA种类相对于未经处理的蠕虫减少至少80％,一些迹象表明可能积累更重的前体分子[1]。

[细胞实验]

将适当量的Hycanthone（1至100μg）在10mL维持培养基中加入含有约3×10 7个LLC-MK2细胞单层的塑料瓶（75cm 2）中，然后在35℃下孵育24小时。倾析维持培养基，并将2mL流感病毒添加到细胞单层上，并在35℃下孵育2小时。感染的多样性约为1.0。除去接种物并向每个烧瓶中加入10mL维持培养基，然后将其在35℃下孵育24小时。倾析出上清液，以100,000g离心1小时，在4℃下用HCl-KCl缓冲液（pH2.0）透析24小时，然后在4℃下对两次磷酸盐缓冲盐水（pH7.1）透析。持续24小时。流体通过过滤器以获得无菌制剂。将样品储存在-80℃直至测定干扰素活性[2]。

[动物实验]

用作最终宿主的雌性远交瑞士白化小鼠在感染时重18至20克。通过将剂量分成两个后腿，肌内给予Hycanthone 0.01mL / g体重，使得每只小鼠接受80mg / kg体重的游离碱。治疗通常在感染后第8周进行[1]。

[参考文献]

[1]. Pica Mattoccia L, et al. Effect of hycanthone administered in vivo upon the incorporation of radioactive precursors into macromolecules of Schistosoma mansoni. Mol Biochem Parasitol. 1983 Jun;8(2):99-107.

[2]. Hahon N, et al. Action of antischistosomal drugs, hycanthone and its analog 1A-4 N-oxide, on viral interferon induction. J Toxicol Environ Health. 1980 Jul;6(4):705-12.

[相关活性小分子]

海恩酮物理化学性质

[ 密度 ]:
1.25g/cm3

[ 沸点 ]:
570.5ºC at 760mmHg

[ 熔点 ]:
approx 143ºC

[ 分子式 ]:
C₂₀H₂₄N₂O₂S

[ 分子量 ]:
356.48200

[ 闪点 ]:
298.9ºC

[ 精确质量 ]:
356.15600

[ PSA ]:
80.81000

[ LogP ]:
3.73370

[ 折射率 ]:
1.658

[ 储存条件 ]:
2-8℃

海恩酮毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: XO1590000

CHEMICAL NAME :: 9H-Thioxanthen-9-one, 1-((2-(diethylamino)ethyl)amino)-4-(hydroxymethyl)-

CAS REGISTRY NUMBER :: 3105-97-3

BEILSTEIN REFERENCE NO. :: 1402722

LAST UPDATED :: 199612

DATA ITEMS CITED :: 67

MOLECULAR FORMULA :: C20-H24-N2-O2-S

MOLECULAR WEIGHT :: 356.52

WISWESSER LINE NOTATION :: T C666 BS IVJ D1Q GM2N2&2

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 980 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 :: 286 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 :: 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 :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1120 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 :: 270 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 :: 70 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 :: Intramuscular

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 253 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 :: Intramuscular

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 180 mg/kg/60D-I

TOXIC EFFECTS :: Tumorigenic - Carcinogenic by RTECS criteria Liver - other changes Liver - tumors

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Parenteral

DOSE :: 50 mg/kg

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

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

TYPE OF TEST :: Sex chromosome loss and nondisjunction

TYPE OF TEST :: Sex chromosome loss and nondisjunction

TYPE OF TEST :: DNA inhibition

TYPE OF TEST :: Mutation test systems - not otherwise specified

TYPE OF TEST :: Cytogenetic analysis

TYPE OF TEST :: Micronucleus test

TYPE OF TEST :: Micronucleus test

TYPE OF TEST :: Specific locus test

TYPE OF TEST :: Specific locus test

TYPE OF TEST :: Cytogenetic analysis

TYPE OF TEST :: Micronucleus test

TYPE OF TEST :: Sister chromatid exchange

TYPE OF TEST :: Sister chromatid exchange

TYPE OF TEST :: Unscheduled DNA synthesis

MUTATION DATA

TYPE OF TEST :: Cytogenetic analysis

TEST SYSTEM :: Rodent - rabbit Leukocyte

DOSE/DURATION :: 5 mg/L

REFERENCE :: MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 55,43,1978 *** REVIEWS *** TOXICOLOGY REVIEW EJBLAB Egyptian Journal of Bilharziasis. (National Information and Documentation Center, Al-Tahrir St., Awqaf P.O. Dokki, Cairo, Egypt) V.1- 1974- Volume(issue)/page/year: 1,181,1974

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海恩酮安全信息

[ 危害码 (欧洲) ]:
T: Toxic;

[ 风险声明 (欧洲) ]:
45-46-20/21/22

[ 海关编码 ]:
2932999099

海恩酮上下游产品

海恩酮上游产品

海恩酮下游产品

海恩酮海关

[ 海关编码 ]: 2932999099

[ 中文概述 ]:
2932999099. 其他仅含氧杂原子的杂环化合物. 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

[ Summary ]:
2932999099. other heterocyclic compounds with oxygen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

海恩酮