Tafenoquine

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Chemical Structure| 106635-80-7 同义名 : WR 238605
CAS号 : 106635-80-7
货号 : A299706
分子式 : C24H28F3N3O3
纯度 : 99%+
分子量 : 463.49
MDL号 : MFCD00598712
存储条件:

Pure form Keep in dark place, inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
描述 The 8-aminoquinoline (8AQ) class of anti-malarial compounds is extremely important in the fight against malaria, as this class of molecules is unique due to the efficacy against relapsing forms of malaria. Tafenoquine (TQ) is an 8-aminoquinoline (8AQ) that is currently in late stage development as an anti-malarial prophylactic agent. In the CYP 2D knock-out mouse model, there was no luminescence signal at either 48 or 72 hr post-infection indicating that TQ at its ED100 (3 mg/kg) prevented P. berghei infection. TQ was tested at two times its ED100 in the humanized/CYP 2D6 knock-in mouse strain. The results showed that there was less luminescence signal in all five mice at 48 hr (as compared to WT-infected controls) and no detectable luminescence signal at 72 hr post-inoculation. Five out of five WT mice treated with TQ had no detectable parasite burden after 31 days, in comparison to the WT infection control or the CYP 2D knock-out mice treated with TQ. Those results illustrated that TQ is active in the presence of the CYP 2D gene cluster[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.16mL

0.43mL

0.22mL

10.79mL

2.16mL

1.08mL

21.58mL

4.32mL

2.16mL

参考文献

[1]Dow G, Smith B. The blood schizonticidal activity of tafenoquine makes an essential contribution to its prophylactic efficacy in nonimmune subjects at the intended dose (200 mg). Malar J. 2017 May 19;16(1):209.

[2]Chu CS, Bancone G, et al. Haemolysis in G6PD Heterozygous Females Treated with Primaquine for Plasmodium vivax Malaria: A Nested Cohort in a Trial of Radical Curative Regimens. PLoS Med. 2017 Feb 7;14(2):e1002224.

[3]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.