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Tafenoquine Succinate

Tafenoquine Succinate用途

Tafenoquine Succinate (WR 238605 Succinate) 是一种 8-氨基喹啉。Tafenoquine 作为抗疟疾预防剂。
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Tafenoquine Succinate名称

[ CAS 号 ]:
106635-81-8

[ 中文名 ]:
Tafenoquine Succinate

[ 英文名 ]:
Tafenoquine (Succinate)

[英文别名 ]:

Tafenoquine Succinate生物活性

[ 描述 ]:

Tafenoquine Succinate (WR 238605 Succinate) 是一种 8-氨基喹啉。Tafenoquine 作为抗疟疾预防剂[1]。

[ 相关类别 ]:

信号通路 >> 抗感染 >> 寄生物
研究领域 >> 感染

[ 靶点 ]

Anti-malarial[1]


[体内研究]

当以在WT小鼠中建立的ED100值(3mg/kg)给药时,Tafenoquine在CYP 2D敲除小鼠中没有表现出抗疟疾活性。当人源化/ CYP 2D6敲入小鼠的ED100(6mg/kg)的两倍测试时,Tafenoquine抗疟疾活性部分恢复[1]。

[参考文献]

[1]. Marcsisin SR, et al. Tafenoquine and NPC-1161B require CYP 2D metabolism for anti-malarial activity: implications for the 8-aminoquinoline class of anti-malarial compounds. Malar J. 2014 Jan 3;13:2.


[相关活性小分子]

硫酸羟基氯喹 | 甲硝唑 | Emetine dihydrochloride hydrate | 伊维菌素 | 青蒿素 | 盐酸左旋咪唑 | 氟雷拉纳 | RRX-001 | 阿维菌素 | 奎尼丁 | 硫双二氯酚 | 氟苯咪唑 | 甲苯咪唑 | SQ109 | 蒿甲醚

Tafenoquine Succinate物理化学性质

[ 密度 ]:
1.237g/cm3

[ 沸点 ]:
565.6ºC at 760mmHg

[ 分子式 ]:
C28H34F3N3O7

[ 分子量 ]:
581.58100

[ 闪点 ]:
295.9ºC

[ 精确质量 ]:
581.23500

[ PSA ]:
153.23000

[ LogP ]:
6.61990

[ 储存条件 ]:
2-8℃

Tafenoquine SuccinateMSDS

Tafenoquine Succinate毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :
SA0242400
CAS REGISTRY NUMBER :
106635-81-8
LAST UPDATED :
199107
DATA ITEMS CITED :
2
MOLECULAR FORMULA :
C24-H28-F3-N3-O3.C4-H6-O4
MOLECULAR WEIGHT :
581.65

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 :
416 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
JMCMAR Journal of Medicinal Chemistry. (American Chemical Soc., Distribution Office Dept. 223, POB POB 57136, West End Stn., Washington, DC 20037) V.6- 1963- Volume(issue)/page/year: 32,1728,1989
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
71 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
JMCMAR Journal of Medicinal Chemistry. (American Chemical Soc., Distribution Office Dept. 223, POB POB 57136, West End Stn., Washington, DC 20037) V.6- 1963- Volume(issue)/page/year: 32,1728,1989
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Tafenoquine Succinate安全信息

[ 危险品运输编码 ]:
NONH for all modes of transport

Tafenoquine Succinate文献

Uptake of the antileishmania drug tafenoquine follows a sterol-dependent diffusion process in Leishmania.

J. Antimicrob. Chemother. 66(11) , 2562-5, (2011)

The present study was designed to elucidate the mechanism of tafenoquine uptake in Leishmania and its sterol dependence.Because tafenoquine is a fluorescent compound, spectrofluorimetric analysis allo...

Transmission-blocking activity of tafenoquine (WR-238605) and artelinic acid against naturally circulating strains of Plasmodium vivax in Thailand.

Am. J. Trop. Med. Hyg. 69(5) , 542-7, (2003)

The sporontocidal activity of tafenoquine (WR-238605) and artelinic acid was determined against naturally circulating isolates of Plasmodium vivax in western Thailand. Primaquine was used as a negativ...

Military aviators, special operations forces, and causal malaria prophylaxis.

Mil. Med. 168(12) , 1001-6, (2003)

U.S. military aviators are currently restricted to the use of chloroquine or doxycycline for malaria prophylaxis. Ground forces are allowed the additional option of taking mefloquine. These medication...


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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

价格:

联系人:徐经理

产品详情:N4-(2,6-二甲氧基-4-甲基-5-(3-(三氟甲基)苯氧基)喹啉-8-基)戊烷-1,4-二胺琥珀酸盐


公司名:上海创赛科技有限公司

区域:上海市嘉定区

价格:
¥4277.0/10mg ¥2851.0/5mg

联系人:夏言

产品详情:[Perfemiker]Tafenoquine Succinate,≥99%


公司名:武汉壹加壹生物科技有限公司

区域:武汉市江夏区

价格:
¥需询单/1kg

联系人:刘经理

产品详情:Tafenoquine Succinate


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