化合物 P163-0892 T61290

Product Introduction
Bioactivity


英文名: P163-0892

描述: P163-0892 is a highly effective and specific antifungal compound targeting Cryptococcus species. Additionally, P163-0892 demonstrates moderate capability to penetrate the blood-brain barrier [1].

体外活性: P163-0892 (0-32 μg/mL, 48 h) shows antifungal activity with a MIC of 0.25 μg/mL and 0.5 μg/mL against Cryptococcus neoformans and Cryptococcus gattii, respectively [1]. P163-0892 has good aqueous solubility [1]. P163-0892 has no cytotoxicity and no obvious cardiotoxicity [1].

体内活性: P163-0892 (10 mg/kg; 5 days) significantly extends the survival of larvae infected with either C. neoformans or C. gattii [1]. Animal Model: Wax moth larva infected with C. neoformans H99 or C. gattii WM178 [1] Dosage: 10 mg/kg Administration: 5 days Result: Increased the survival rate of larvae. Animal Model: Male Sprague–Dawley rats weighing 200–250 g [1] Dosage: 2 mg/kg or 5 mg/kg Administration: Intravenous or oral administration (Pharmacokinetic Analysis) Result: Pharmacokinetic Parameters of P163-0892 a route dose (mg/kg) C 0 (ng/mL) C max (ng/mL) T 1/2 (h) T max (h) AUC 0-inf (h ng/mL) Cl (mL/h/kg) MRT 0-t (h) Vd ss (L/kg) BA (%) iv 2 mg/kg 2460 7.61 749 172 2.63 7.12 po 5 mg/kg 2.97 15.3 3.17 NR

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途