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Merck
CN

SML0396

Sigma-Aldrich

Tafenoquine succinate

≥95% (HPLC)

别名:

N-[2,6-Dimethoxy-4-methyl-5-[3-(trifluoromethyl)phenoxy]quinolin-8-yl]pentane-1,4-diamine, SB-252263, WR 238605

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About This Item

经验公式(希尔记法):
C24H28F3N3O3 · C4H6O4
分子量:
581.58
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77

质量水平

检测方案

≥95% (HPLC)

形式

powder

储存条件

desiccated

颜色

white to beige

溶解性

DMSO: 5 mg/mL (clear solution)

储存温度

2-8°C

SMILES字符串

OC(=O)CCC(O)=O.COc1cc(C)c2c(Oc3cccc(c3)C(F)(F)F)c(OC)cc(NC(C)CCCN)c2n1

InChI

1S/C24H28F3N3O3.C4H6O4/c1-14-11-20(32-4)30-22-18(29-15(2)7-6-10-28)13-19(31-3)23(21(14)22)33-17-9-5-8-16(12-17)24(25,26)27;5-3(6)1-2-4(7)8/h5,8-9,11-13,15,29H,6-7,10,28H2,1-4H3;1-2H2,(H,5,6)(H,7,8)

InChI key

CQBKFGJRAOXYIP-UHFFFAOYSA-N

生化/生理作用

Tafenoquine has been generally generated for oral administration and drug absorption increases when taken along with food. It is known to possess a longer half life.
Tafenoquine is an antimalarial primaquine analog being investigated to treat and prevent Plasmodium vivax infections. It can eliminate both blood and liver stages of Plasmodium vivax. Tafenoquine has also been tested as a therapy for leishmaniasis.

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

法规信息

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Travelers' Malaria, 172-172 (2008)
Douglas S Walsh et al.
The Journal of infectious diseases, 190(8), 1456-1463 (2004-09-21)
We assessed monthly doses of tafenoquine for preventing Plasmodium vivax and multidrug-resistant P. falciparum malaria. In a randomized, double-blind, placebo-controlled study, 205 Thai soldiers received either a loading dose of tafenoquine 400 mg (base) daily for 3 days, followed by
Bruce G Charles et al.
Antimicrobial agents and chemotherapy, 51(8), 2709-2715 (2007-05-23)
The population pharmacokinetics of tafenoquine were studied in Australian soldiers taking tafenoquine for malarial prophylaxis. The subjects (476 males and 14 females) received a loading dose of 200 mg tafenoquine base daily for 3 days, followed by a weekly dose
Maryanne Crockett et al.
Expert opinion on investigational drugs, 16(5), 705-715 (2007-04-28)
Malaria remains an important cause of global morbidity and mortality. As antimalarial drug resistance escalates, new safe and effective medications are necessary to prevent and treat malarial infection. Tafenoquine is an 8-aminoquinoline antimalarial that is presently under development. It has
Akintunde Sowunmi et al.
Chemotherapy, 57(6), 497-504 (2012-01-21)
Artemisinin-based combination treatments (ACTs) are the recommended first-line antimalarials globally, but their influence on the risk factors associated with gametocyte carriage has had little evaluation in endemic areas. The risk factors associated with gametocytaemia at presentation and after ACTs were

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