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CRK12-IN-1

CAS No. : 1990479-14-5

MCE 站：CRK12-IN-1

产品活性：CRK12-IN-1 是一种有效的 CRK12 抑制剂。CRK12-IN-1 对布氏锥虫 (T.b. brucei) 有强效抗性，能迅速杀死病原细胞，对刚果锥虫 ( T. congolense) 也同样有效 (EC₅₀ 分别为1.3和18 nM)。

研究领域：Anti-infection

作用靶点：Parasite

In Vitro: 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).

In Vivo: 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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