BDA-410

BDA-410 is a cysteine protease inhibitor with ki values of 130 nM and 630 nM for calpain-1 and calpain-2, respevtively. BDA-410 inhibits recombinant falcipain-2B with an IC50 of 628 nM and exhibits anti-malarial effects[1].

Research Areas >> Infection

Signaling Pathways >> Metabolic Enzyme/Protease >> Proteasome

ki: 130 nM (Calpain-1), 630 nM (Calpain-2)[1] IC50: 628 nM (Recombinant falcipain-2B)[1]

BDA-410 inhibits malaria parasite growth in vitro with an IC50 value of 173 nM[1].

BDA-410 (25 mg/kg; i.p. injection for three times per day; 4 days) rapidly clears parasitemia in vivo resulting in ~72% inhibition with no obvious detrimental effects due to inhibitor treatment in infected mice. All BDA-410 treated mice survive for longer[1]. Animal Model: C57BL/6 mice (4-6 weeks of age, 20-22g of weight)[1] Dosage: 25 mg/kg Administration: Given i.p. injection; three times per day for 4 days Result: Rapidly cleared parasitemia in vivo resulting in ~72% inhibition with no obvious detrimental effects due to inhibitor treatment in infected mice.BDA-410 treated mice survived until around day 23 compared with control group; and two of the eight BDA-410 treated mice survived until day 60.

[1]. Xuerong Li, et al. BDA-410: A novel synthetic calpain inhibitor active against blood stage malaria. Mol Biochem Parasitol. 2007 Sep; 155(1): 26–32.