产品
编 号：F753535
分子式：C18H20N6O2S
分子量：384.46
分子式：C18H20N6O2S
分子量：384.46
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CAS No: 2516237-50-4
产品详情
生物活性：
Antiparasitic agent-9 (compound 47) is an orally active and potent antiparasitic agent. Antiparasitic agent-9 shows antiparasitic activity against the human parasite.
体内研究：
Antiparasitic agent-9 (compound 47) (15 mg/kg, Orally, twice each day for 7 days) reduces adult worm burden in the jird L. sigmodontis infection model.Antiparasitic agent-9 (2 mg/kg (IV), 10 and 30 mg/kg (PO); once) shows a brain to plasma ratio of 0.08, suggesting limited brain exposure.Pharmacokinetic Parameters of Antiparasitic agent-9 in male Male CD-1 mouse.PO (30 mg/kg) PO (10 mg/kg) IV (2 mg/kg)
Cmax (μM)13.95.27 ± 0.83
Tmax (h)0.504.0 ± 2.8
AUC0-inf (μM·h)12168.1±NC
CL (mL/min/kg)3.6 ± 0.22
Vd ss (mL/kg)0.74 ± 0.08
F (%)57
brain/plasma [b]/[p]0.08
efflux ratio (ER)12
Animal Model:Female BALB/c mice (infected withL. sigmodontis, 6-8 weeks)
Dosage:15 mg/kg
Administration:Orally, twice each day for 7 days
Result:Showed a significant worm burden reduction of 59% at 15 mg/kg.
Animal Model:Male CD-1 mouse (n = 4)
Dosage:2 mg/kg (IV), 10 and 30 mg/kg (PO)
Administration:IV, PO, once (Pharmacokinetic Analysis)
Result:Showed a brain to plasma ratio of 0.08, suggesting limited brain exposure.
Antiparasitic agent-9 (compound 47) is an orally active and potent antiparasitic agent. Antiparasitic agent-9 shows antiparasitic activity against the human parasite.
体内研究：
Antiparasitic agent-9 (compound 47) (15 mg/kg, Orally, twice each day for 7 days) reduces adult worm burden in the jird L. sigmodontis infection model.Antiparasitic agent-9 (2 mg/kg (IV), 10 and 30 mg/kg (PO); once) shows a brain to plasma ratio of 0.08, suggesting limited brain exposure.Pharmacokinetic Parameters of Antiparasitic agent-9 in male Male CD-1 mouse.PO (30 mg/kg) PO (10 mg/kg) IV (2 mg/kg)
Cmax (μM)13.95.27 ± 0.83
Tmax (h)0.504.0 ± 2.8
AUC0-inf (μM·h)12168.1±NC
CL (mL/min/kg)3.6 ± 0.22
Vd ss (mL/kg)0.74 ± 0.08
F (%)57
brain/plasma [b]/[p]0.08
efflux ratio (ER)12
Animal Model:Female BALB/c mice (infected withL. sigmodontis, 6-8 weeks)
Dosage:15 mg/kg
Administration:Orally, twice each day for 7 days
Result:Showed a significant worm burden reduction of 59% at 15 mg/kg.
Animal Model:Male CD-1 mouse (n = 4)
Dosage:2 mg/kg (IV), 10 and 30 mg/kg (PO)
Administration:IV, PO, once (Pharmacokinetic Analysis)
Result:Showed a brain to plasma ratio of 0.08, suggesting limited brain exposure.
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