CRK12-IN-1

Research use only, not for human use.

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

CRK12-IN-1 is a potent CRK12 inhibitor. CRK12-IN-1 is extremely potent against T.b. brucei and rapidly cytocidal, as well as equally potent against T. congolense and T. vivax (EC50 of 1.3 and 18 nM, respectively).

CRK12-IN-1 (compound 1) (10 mg/mL; 69 hours) is extremely potent against T.b. brucei and in animal models of T.b. brucei infection, as well as a potent inhibitor of T. congolensei (EC50 of 1.3 and 18 nM, respectively)..

CRK12-IN-1 (compound 1) (50 or 10 mg/kg; s.c.; once daily for 4 days) can elicit sterile cure in 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.CRK12-IN-1 (5 mg/kg, s.c., twice 12 h apart for 4 days) can suppress parasitaemia below the level of detection in T. congolense infected calves, but parasitaemia quickly re-emerges following the cessation of treatment.CRK12-IN-1 (10 mg free base/kg; s.c.; for 0.08-8 hours) has 74% of bioavailability with a half-life of about 1 hour in female NMRI mice.CRK12-IN-1 (i.m. at 5 mg free base/kg or i.v. at 2.5 mg free base/kg; 0.25-120 hours) 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.

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Microbiology/Virology

Antibiotic

Antibiotic

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1990479-14-5

472.57

C20H26F2N4O3S2

>98% (HPLC)

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C(=O)(C=1SC(N[C@@H]2CC[C@@H](NS(CC(C)C)(=O)=O)CC2)=NC1N)C3=C(F)C=CC=C3F

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(-20℃)

With Ice Pack

≥ 2 years