INE963

Research use only, not for human use.

INE963 demonstrates potent cellular activity against Pf 3D7 (EC50 = 6 nM) and achieves "artemisinin-like" kill kinetics in vitro with a parasite clearance time of <24 h.

INE963 demonstrates potent cellular activity against Pf 3D7 (EC50 = 6 nM) and achieves "artemisinin-like" kill kinetics in vitro with a parasite clearance time of <24 h. INE963 is also potent against P. falciparum and P. vivax clinical isolates from Brazil and Uganda with EC50’s ranging from 0.01 to 7.0 nM(In Vitro):INE963 is active against >15 drug-resistant Pf cell lines with EC50’s = 0.5–15 nM. The in vitro log parasite reduction ratio for INE963 is >8.0 at 10 × Pf 3D7 EC50 without a lag phase and a parasite clearance time (PCT99.9) of <24 h. The in vitro selectivity of INE963for Plasmodium vs human cells was exemplified by approximately 1000+ fold shifts against multiple human kinase biochemical assays.(In Vivo):Following four oral doses at 30 mg/kg of INE963, the frontrunner compounds tested showed significant parasitemia reduction (>99.9%) at day 5 compared to untreated control mice. In addition, the animals did not show any signs of recrudescence of parasite at day 60 post-treatment, indicating complete cure at these doses.

——

——

——

Others

Other Targets

Human Endogenous Metabolite

——

——

2640567-43-5

402.51

C19H26N6O2S

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (248.44 mM)

CC(C)c(cc1)nc(OC)c1-c1cnc2sc(N(CC3)CCC3(CN)O)nn12

——

(-20℃)

With Ice Pack

≥ 2 years