| Bioactivity | GNF179 is an optimized 8,8-dimethyl imidazolopiperazine analog that exhibits antimalarial potency (IC50 of 4.8 nM against the multidrug resistant strain W2). GNF179 is orally active[1]. | ||||||||||||
| Invitro | GNF179 不会快速抑制寄生虫蛋白质的生物合成，也不太可能靶向寄生虫细胞色素 bc1，细胞色素 bc1 是 Atovaquone (HY-13832) 的肝脏阶段靶点。 GNF179 可能对孢子体而不是在肝阶段起作用[1]。GNF179 (5-100 nM; 48 h) 在 5 nM 时消除卵囊形成，对蚊子配子细胞的性生活周期进程具有高度抑制作用[2]。 | ||||||||||||
| In Vivo | GNF179 (15 mg/kg; p.o.; single dose) 在啮齿动物疟疾模型中显示抗疟活性[1]。 Animal Model: | ||||||||||||
| Name | GNF179 | ||||||||||||
| CAS | 1261114-01-5 | ||||||||||||
| Formula | C22H23ClFN5O | ||||||||||||
| Molar Mass | 427.90 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Meister S, et al. Imaging of Plasmodium liver stages to drive next-generation antimalarial drug discovery. Science. 2011 Dec 9;334(6061):1372-7. [2]. Ouologuem DT, et al. A Novel Ex Vivo Drug Assay for Assessing the Transmission-Blocking Activity of Compounds on Field-Isolated Plasmodium falciparum Gametocytes. Antimicrob Agents Chemother. 2022 Nov 2:e0100122. |
GNF179
CAS: 1261114-01-5 F: C22H23ClFN5O W: 427.90
GNF179 is an optimized 8,8-dimethyl imidazolopiperazine analog that exhibits antimalarial potency (IC50 of 4.8 nM agains
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