HSP90-IN-9,2765247-36-5

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HSP90-IN-9

CAS No. : 2765247-36-5

MCE 国际站：HSP90-IN-9

产品活性：HSP90-IN-9 是一种有效的选择性 HSP90 抑制剂。HSP90-IN-9 以剂量依赖性方式显示杀真菌作用。HSP90-IN-9 与 FLC 联合用药可抑制真菌生物膜形成和真菌形态变化。HSP90-IN-9 可通过下调 ERG11、CDR1 和 CDR2 基因表达恢复对 FLC 的耐药性。

研究领域：Cell Cycle/DNA Damage  |  Metabolic Enzyme/Protease  |  Anti-infection

作用靶点：HSP  |  Fungal

In Vitro: HSP90-IN-9 (compound A17) (combined with FLC (2 µg/mL)) shows antifungal activities against the six FLC-resistant Candida albicans (C. albicans) strains (MIC₈₀s of 0.125 µg/mL in strain 901, strain 632, strain 100; MIC₈₀s of 0.25 µg/mL in strain 904, strain 103,strain311, respectively).
HSP90-IN-9 (24 h) shows low toxic to human cancer cells, human normal cells and the macrophage lineage (IC₅₀s is 13.12, 34.09, 17.45, 7.15, >50, 21.33, 17.05, 10.34 µM in A549, MCF-7, HEPG2, THLE-2, BEAS-2B, NIH-3T3, Raw264.7, BV-2 cells, respectively).
HSP90-IN-9 (32 μg/mL (combined with FLC (32 μg/mL)), 24 h) inhibits fungal biofilm formation and fungal morphological changes after being combined with FLC.
HSP90-IN-9 (C. albicans (strain 904), 48 h) displays a fungicidal effect in a dose-dependent manner.
HSP90-IN-9 (FLC + compound A17 (32 + 32 μg/mL)) recovers azole sensitivity in resistant C.albicans by down-regulating the expression of CYP51 (ERG11) efflux pump-related genes (CDR1 and CDR2).

In Vivo: HSP90-IN-9 (10 mg/kg; i.v.) exhibits moderate pharmacokinetic properties in SD rats.
HSP90-IN-9 (A17 (10 mg/kg)+FLC (1 mg/kg); i.p.; once a day for 5 days) exhibits potent in vivo antifungal efficacy by reducing the colonization and dissemination of fungi in tissue.
Pharmacokinetic Parameters of HSP90-IN-9 in male Sprague-Dawley (SD) rats.

dose (mg/kg)	T1/2 (h)	C0 (ng/mL)	AUC(0-t) (h*ng/mL)	AUC(0-∞) (h*ng/mL)	Vz (L/kg)	Cl (mL/min/kg)	MRT(0-∞) (h)
10 mg/kg	1.26±0.31	4752.50±44.54	3005.15±35.59	3028.95±54.14	11.25±3.69	101.77±1.96	1.12±0.07

male Sprague-Dawley (SD) rats; 10 mg/kg; i.v.

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