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 HDAC 亚型。

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 [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]. Animal Model: P. falciparum Pf3D 70087/N9 in NODscidIL2Rγ null mice (engrafted with human erythrocytes) [1] Dosage: 10 and 50 mg/kg Administration: P.o.; bw for 4 days Result: Resulted in a significant reduction in parasitaemia with 6.5% and 2.57% parasitaemia at 10 and 50 mg/kg, respectively.

C21H24ClN5O2

413.9

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years