Antiparasitic agent-9 (compound 47) 是一种口服有效的抗寄生虫剂。Antiparasitic agent-9 显示对人类寄生虫的抗寄生虫活性。
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Antiparasitic agent-9 (compound 47) is an orally active and potent antiparasitic agent. Antiparasitic agent-9 shows antiparasitic activity against the human parasite [1].
体内活性
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 [1]. 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 [1]. Animal Model: Female BALB/c mice (infected with L. sigmodontis, 6-8 weeks) [1] 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) [1] Dosage: 2 mg/kg (IV), 10 and 30 mg/kg (PO) Administration: IV, PO, once (Pharmacokinetic Analysis) Result: Pharmacokinetic Parameters of Antiparasitic agent-9 in male Male CD-1 mouse [1]. PO (30 mg/kg) PO (10 mg/kg) IV (2 mg/kg) C max (μM) 13.9 5.27 ± 0.83 T max (h) 0.50 4.0 ± 2.8 AUC 0-inf (μM·h) 121 68.1±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
Cas No.
2516237-50-4
分子式
C18H20N6O2S
分子量
384.46
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years