产品说明书
Tafenoquine Succinate
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同义名 : | WR 238605 Succinate |
| CAS号 : | 106635-81-8 | |
| 货号 : | A1143148 | |
| 分子式 : | C28H34F3N3O7 | |
| 纯度 : | 99%+ | |
| 分子量 : | 581.581 | |
| MDL号 : | MFCD00892249 | |
| 存储条件： |
粉末 Keep in dark place,Inert atmosphere,Room temperature 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 120 mg/mL(206.33 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
| 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]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
1.72mL 0.34mL 0.17mL |
8.60mL 1.72mL 0.86mL |
17.19mL 3.44mL 1.72mL |
| 参考文献 |
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[2]Chen V, Daily JP. Tafenoquine: the new kid on the block. Curr Opin Infect Dis. 2019;32(5):407-412 |