P163-0892 是一种对Cryptococcus种具有强选择性的抗真菌剂(Antifungal)。P163-0892 被预测具有中等程度的血脑屏障穿透性。
产品描述
P163-0892 is a potent and selective antifungal agent against Cryptococcus species. P163-0892 is predicted to show medium BBB penetration [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
Cas No.
1574576-45-6
分子式
C19H20N2O3S
分子量
356.44
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