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编 号:F748225
分子式:C23H33F2N5O3S2
分子量:529.67
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生物活性:
CRK12-IN-2 (compound 2) is an inhibitor of CRK12. CRK12-IN-2 shows potency against Trypanosoma congolense and Trypanosoma vivax with EC50 values of 3.2 and 0.08 nM. CRK12-IN-2 can be used for the research of animal trypanosomiasis.

体内研究:
CRK12-IN-2 (10 mg/kg; s.c. once daily for 4 days) effectively cures mice with T. congolense- and T. vivax-infection.1.19Pharmacokinetic Properties of CRK12-IN-2 in Cattle.CattleIV 2 mg/kg CattleIM 10 mg/kg
Clb (mL/min/kg)15±5
Vdss (L/kg)2.3±0.6
half-life (h)4±2
AUC0-∞(ng·min/mL)140000±40000500000±30000
Cmax (ng/mL) 1700±800
Tmax (h) 1.3±0.6
F (%) 73±6
Animal Model:Mice with T. congolense and T. vivax infection
Dosage:10 mg/kg
Administration:Subcutaneous injection; 10 mg/kg once daily; for 4 days
Result:Fully cured both T. congolense- and T. vivax-infected mice for 4 days at a dose of 10 mg/kg.
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