产品
编 号：F755762
分子式：C30H31N3O5
分子量：513.58
分子式：C30H31N3O5
分子量：513.58
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CAS No: 2765247-36-5
产品详情
生物活性：
HSP90-IN-9 is a potent and selective HSP90 inhibitor. HSP90-IN-9 displays a fungicidal effect in a dose-dependent manner. HSP90-IN-9 inhibits fungal biofilm formation and fungal morphological changes after being combined with FLC. HSP90-IN-9 recovers FLC resistance by down-regulating the expression of related genes (ERG11, CDR1 and CDR2).
体内研究：
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/kg1.26±0.314752.50±44.543005.15±35.593028.95±54.1411.25±3.69101.77±1.961.12±0.07
male Sprague-Dawley (SD) rats; 10 mg/kg; i.v.Animal Model:male Sprague-Dawley (SD) rats
Dosage:10 mg/kg
Administration:i.v.
Result:Exhibited moderate pharmacokinetic properties in SD rats.
Animal Model:female SD rats, 160-180 g (IFI rat model)
Dosage:10 mg/kg, A17 (10 mg/kg)+FLC (1 mg/kg)
Administration:i.p., once a day, 5 days
Result:Exhibited potent in vivo antifungal efficacy by reducing the colonization and dissemination of fungi in tissue.
体外研究：
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).
HSP90-IN-9 is a potent and selective HSP90 inhibitor. HSP90-IN-9 displays a fungicidal effect in a dose-dependent manner. HSP90-IN-9 inhibits fungal biofilm formation and fungal morphological changes after being combined with FLC. HSP90-IN-9 recovers FLC resistance by down-regulating the expression of related genes (ERG11, CDR1 and CDR2).
体内研究：
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/kg1.26±0.314752.50±44.543005.15±35.593028.95±54.1411.25±3.69101.77±1.961.12±0.07
male Sprague-Dawley (SD) rats; 10 mg/kg; i.v.Animal Model:male Sprague-Dawley (SD) rats
Dosage:10 mg/kg
Administration:i.v.
Result:Exhibited moderate pharmacokinetic properties in SD rats.
Animal Model:female SD rats, 160-180 g (IFI rat model)
Dosage:10 mg/kg, A17 (10 mg/kg)+FLC (1 mg/kg)
Administration:i.p., once a day, 5 days
Result:Exhibited potent in vivo antifungal efficacy by reducing the colonization and dissemination of fungi in tissue.
体外研究：
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).
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