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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。

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
UNII-DL5J0B8VSS
Tafenoquine Succinate
tafenoquine maleate
Etaquine
Tafenoquine (Succinate)

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]

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

详细MSDS(安全技术说明书)

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

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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