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FNDR-20123 free base, a pioneering and orally administered anti-malarial agent, acts as a Histone Deacetylase (HDAC) inhibitor, displaying potent efficacy with IC50 values of 31 nM for Plasmodium and 3 nM for human HDAC, respectively. It effectively targets both the asexual (IC50=41 nM) and sexual blood stages (IC50=190 nM for male gametocytes) of Plasmodium falciparum. Additionally, FNDR-20123 free base inhibits multiple HDAC isoforms, namely HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8, with respective IC50 values of 25, 29, 2, 11, and 282 nM, and displays nanomolar inhibitory concentrations against Class III HDAC isoforms [1].
Pack Size | Price | Availability | Quantity |
---|---|---|---|
25 mg | $1,520 | 6-8 weeks | |
50 mg | $1,980 | 6-8 weeks | |
100 mg | $2,500 | 6-8 weeks |
Description | FNDR-20123 free base, a pioneering and orally administered anti-malarial agent, acts as a Histone Deacetylase (HDAC) inhibitor, displaying potent efficacy with IC50 values of 31 nM for Plasmodium and 3 nM for human HDAC, respectively. It effectively targets both the asexual (IC50=41 nM) and sexual blood stages (IC50=190 nM for male gametocytes) of Plasmodium falciparum. Additionally, FNDR-20123 free base inhibits multiple HDAC isoforms, namely HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8, with respective IC50 values of 25, 29, 2, 11, and 282 nM, and displays nanomolar inhibitory concentrations against Class III HDAC isoforms [1]. |
In vitro | FNDR-20123 demonstrates activity against all tested resistant strains, offering significant potential for eradicating the swiftly evolving drug-resistant parasite [1]. |
In vivo | FNDR-20123, administered orally at dosages of 10 to 50 mg/kg body weight over a period of four days, significantly reduced parasitemia in a P. falciparum mouse model [1]. This model involved NODscidIL2Rγ null mice engrafted with human erythrocytes, simulating P. falciparum Pf3D 70087/N9 infection. The administration led to a noteworthy decrease in parasitemia levels, showing 6.5% and 2.57% at dosages of 10 mg/kg and 50 mg/kg, respectively. |
Molecular Weight | 377.44 |
Formula | C21H23N5O2 |
Cas No. | 1267502-34-0 |
Storage | Shipping with blue ice. |
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