CRK12-IN-1 is a potent CRK12 inhibitor.CRK12-IN-1 has insecticidal activity, with inhibitory effects on Trypanosoma brucei (T.b. brucei) and Trypanosoma congolense (T. congolense) with EC50s of 1.3 and 18 nM, respectively.CRK12-IN-1 kills the pathogenic cells rapidly.

CRK12-IN-1(compound 1) (10 mg/mL; 69 h) demonstrates exceptional potency against T.b. brucei, proving highly effective in animal models of T.b. brucei infection. Additionally, it serves as a potent inhibitor of T. congolensei, with EC50 values of 1.3 and 18 nM, respectively.[1]

CRK12-IN-1 (compound 1) (5 mg free base/kg, i.m. or 2.5 mg free base/kg, i.v.; 0.25-120 h) has a moderate clearance from the blood and a relatively short half-life (about1.8 h) in male ruminating Holstein-Friesian, and penetrate tissues beyond the vasculature.[1]
CRK12-IN-1 (5 mg/kg; s.c.; twice 12 h apart for 4 days) can suppress parasitemia below the level of detection in T. congolense infected calves, but parasitemia quickly re-emerges following the cessation of treatment.[1]
CRK12-IN-1 (10 mg free base/kg; s.c.; for 0.08-8 h) has 74% of bioavailability with a half-life of about 1 hour in female NMRI mice.[1]
CRK12-IN-1 (50 or 10 mg/kg; s.c.; once daily for 4 days) can elicit sterile cure against T. congolense infected mice, also has the same effect but marginally more efficacious (30 or 3 mg/kg; s.c.; daily, for 4 days) in against T. vivax infected mice.[1]