|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|CsnPharm

CAS No.: 106635-81-8

Tafenoquine Succinate/他非诺喹琥珀酸盐 Catalog No. CSN23845

Synonyms: WR 238605 (Succinate);WR-238605;SB-252263-AAB

Tafenoquine Succinate (WR 238605 Succinate) is an 8-aminoquinoline. Tafenoquine is an anti-malarial prophylactic agent[1].

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技术信息

生物活性

描述Tafenoquine Succinate (TQ) is an 8-aminoquinoline (8AQ) and an anti-malarial prophylactic agent. NPC-1161B and TQ exhibited no anti-malarial activity in CYP 2D knock-out mice when dosed at their ED100 values (1 mg/kg and 3 mg/kg, respectively) established in WT mice. TQ anti-malarial activity was partially restored in humanized/CYP 2D6 knock-in mice when tested at two times its ED100^[1]. Single-dose tafenoquine provides equivalent efficacy to 14 days of primaquine for radical cure in P. vivax, and it can be dosed weekly to prevent malaria^[2]. Single-dose tafenoquine resulted in a significantly lower risk of P. vivax recurrence than placebo in patients with phenotypically normal G6PD activity^[3]. Tafenoquine is effective for both primary and terminal prophylaxis. If used for primary prophylaxis it may continue to offer protection against vivax relapses after exposure has ended (as terminal prophylaxis)^[4].
参考文献

[1] Marcsisin SR, Sousa JC, Reichard GA, 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;13:2.
[2] Chen V, Daily JP. Tafenoquine: the new kid on the block. Curr Opin Infect Dis. 2019;32(5):407-412
[3] Lacerda MVG, Llanos-Cuentas A, Krudsood S, et al. Single-Dose Tafenoquine to Prevent Relapse of Plasmodium vivax Malaria. N Engl J Med. 2019;380(3):215-228
[4] Rodrigo C, Rajapakse S, Fernando SD. Tafenoquine for primary and terminal prophylaxis of malaria in apparently healthy people: a systematic review. Trans R Soc Trop Med Hyg. 2019;113(10):579-586

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.7195 mL
- 8.5973 mL
- 17.1945 mL
- 5 mM
- 0.3439 mL
- 1.7195 mL
- 3.4389 mL
- 10 mM
- 0.1719 mL
- 0.8597 mL
- 1.7195 mL

技术信息

CAS号

106635-81-8

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C28H34F3N3O7

运输

蓝冰

分子量

581.58

别名

WR 238605 (Succinate);WR-238605;SB-252263-AAB;Krintafel;他非诺喹琥珀酸盐;WR 238605 (Succinate

溶解度

DMSO	120.0 mg/mL (206.3 mM) warming

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Tafenoquine Succinate/他非诺喹琥珀酸盐 Catalog No. CSN23845

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