FNDR-20123
目录号: PL03238 纯度: ≥98%
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中文名称
FNDR-20123
英文名称
FNDR-20123
包装储存
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
产品详情
FNDR-20123 是一种有效、安全、首创的抗疟疾 HDAC 抑制剂,对疟原虫和人类 HDAC 的 IC50 分别为 31 nM 和 3 nM。FNDR-20123 对恶性疟原虫 (Plasmodium falciparum) 无性期 (IC50=41 nM) 和性血期 (雄性配子体 IC50=190 nM) 具有抗疟疾活性。FNDR-20123 抑制 HDAC1,HDAC2,HDAC3,HDAC6,HDAC8 的 IC50 分别为 25,29,2,11,282 nM,并在纳摩尔浓度下抑制 III 类
生物活性
FNDR-20123 is a safe, first-in-class, and orally active anti-malarial HDAC inhibitor with IC 50 s of 31 nM and 3 nM for Plasmodium and human HDAC, respectively. FNDR-20123 exerts anti-malarial activity against Plasmodium falciparum asexual stage (IC 50 =41 nM) and sexual blood stage (IC 50 =190 nM for male gametocytes). FNDR-20123 inhibits HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8 (IC 50 =25/29/2/11/282 nM, respectively.) and inhibits Class III HDAC isoforms at nanomolar concentrations.
性状
Solid
IC50 & Target[1][2]
human HDAC 3 nM (IC50) Plasmodium HDAC
体外研究(In Vitro)
FNDR-20123 is active against all resistant strains tested so far, which will be highly valuable in eliminating the rapidly evolving drug-resistant parasite. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
FNDR-20123 (10-50 mg/kg; p.o.; bw for 4 days) is also able to reduce parasitaemia significantly in a mouse model for P. falciparum infection. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献
[1]. Potluri V, et al. Discovery of FNDR-20123, a histone deacetylase inhibitor for the treatment of Plasmodium falciparum malaria. Malar J. 2020;19(1):365. Published 2020 Oct 12.
溶解度数据
In Vitro: DMSO : 31.25 mg/mL (75.50 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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