FNDR-20123

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

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库存: 现货

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数量
5mg

￥4100.00

3280.00

- +
10mg

￥6475.00

5180.00

- +
25mg

￥12287.00

9830.00

- +
50mg

￥19237.00

15390.00

- +
100mg

￥30450.00

24360.00

- +

已选 0 种 0 瓶

金额: ￥0.00

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货号: ajcx33766
CAS: 2641930-61-0
别名:
分子式: C21H24ClN5O2
分子量: 413.9
纯度: >98%
溶解度: DMSO : 31.25 mg/mL (75.50 mM; Need ultrasonic)
储存: Store at -20°C
库存: 现货

Background

FNDR-20123 is a safe, first-in-class, and orally active anti-malarial HDAC inhibitor with IC50s of 31 nM and 3 nM for Plasmodium and human HDAC, respectively. FNDR-20123 exerts anti-malarial activity against Plasmodium falciparum asexual stage (IC50=41 nM) and sexual blood stage (IC50=190 nM for male gametocytes). FNDR-20123 inhibits HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8 (IC50=25/29/2/11/282 nM, respectively.) and inhibits Class III HDAC isoforms at nanomolar concentrations[1].

FNDR-20123 is active against all resistant strains tested so far, which will be highly valuable in eliminating the rapidly evolving drug-resistant parasite[1].

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[1].

[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.