产品
编 号：F026512
分子式：C35H38N2O6
分子量：582.69
分子式：C35H38N2O6
分子量：582.69
产品类型
规格
价格
是否有货
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
结构图
CAS No: 1069046-00-9
产品详情
生物活性：
ASB14780 is a 4-phenoxy derivative, the cytosolic Phospholipase A2α (cPLA2α) inhibitor, with an IC50 value of 20 nM.
体内研究：
TPA (tetradecanoyl phorbol acetate) causes acute inflammation with ear, resulting in edema.ASB14780 (50 mg/kg; p.o.; once) suppresses the increase in the ear thickness elicited by the application of TPA (tetradecanoyl phorbol acetate) in mouse.ASB14780 (5 mg/kg; 20 mg/kg; p.o.; once daily) attenuates AHR (airway hyperreactivity), and inhibits IAR (immediate asthmatic response) and LAR (late asthmatic response) in a dose-dependent manner.ASB14780 shows well oral activity of 89.6% in mouse calculated from the ratio of oral administration’s AUC (10 mg/kg; p.o.) and intravenonous administration’s AUC (1 mg/kg; i.v.).Oral Bioavailabilities and Pharmacokinetic Parameters of ASB14780ModelF (%)AUC (h?μg/mL)Cmax (μg/mL)
mouse89.67.125.12
dog34.317.14.96
monkey30.94.962.29
Note: Based on 10 mg/kg p.o. dosing data.Animal Model:TPA (Tetradecanoyl Phorbol Acetate)-induced Ear Edema Model in mouse (female C57BL/6 mice)
Dosage:50 mg/kg
Administration:Oral gavage; 30 min before TPA stimulation
Result:Showed high potency and inhibited ear swelling by 30% and indicated the in vivo anti-inflammatory activity.
Animal Model:Guinea Pig Ovalbumin (OVA)-induced Asthma Model
Dosage:5 mg/kg, 20 mg/kg
Administration:Oral gavage; two single doses; 1 h before and 8 h after passively sensitized administration
Result:Exhibits suppression on IAR (immediate asthmatic response) and LAR (late asthmatic response) in a dose-dependent manner.
体外研究：
ASB14780 shows selectivity to cPLA2α (IC50 =20 nM) over type II sPLA2 (IC50 >10 μM).ASB14780 (30 min pre-incucation) inhibits cPLA2α in guinea pig whole blood (GWB) and human whole blood (HWB) in a species-derived differences, with IC50s of 0.54 μM and 0.64 μM, respectively, 15 min after being stimulated by 5 μM calcium ionophore A23187.
ASB14780 is a 4-phenoxy derivative, the cytosolic Phospholipase A2α (cPLA2α) inhibitor, with an IC50 value of 20 nM.
体内研究：
TPA (tetradecanoyl phorbol acetate) causes acute inflammation with ear, resulting in edema.ASB14780 (50 mg/kg; p.o.; once) suppresses the increase in the ear thickness elicited by the application of TPA (tetradecanoyl phorbol acetate) in mouse.ASB14780 (5 mg/kg; 20 mg/kg; p.o.; once daily) attenuates AHR (airway hyperreactivity), and inhibits IAR (immediate asthmatic response) and LAR (late asthmatic response) in a dose-dependent manner.ASB14780 shows well oral activity of 89.6% in mouse calculated from the ratio of oral administration’s AUC (10 mg/kg; p.o.) and intravenonous administration’s AUC (1 mg/kg; i.v.).Oral Bioavailabilities and Pharmacokinetic Parameters of ASB14780ModelF (%)AUC (h?μg/mL)Cmax (μg/mL)
mouse89.67.125.12
dog34.317.14.96
monkey30.94.962.29
Note: Based on 10 mg/kg p.o. dosing data.Animal Model:TPA (Tetradecanoyl Phorbol Acetate)-induced Ear Edema Model in mouse (female C57BL/6 mice)
Dosage:50 mg/kg
Administration:Oral gavage; 30 min before TPA stimulation
Result:Showed high potency and inhibited ear swelling by 30% and indicated the in vivo anti-inflammatory activity.
Animal Model:Guinea Pig Ovalbumin (OVA)-induced Asthma Model
Dosage:5 mg/kg, 20 mg/kg
Administration:Oral gavage; two single doses; 1 h before and 8 h after passively sensitized administration
Result:Exhibits suppression on IAR (immediate asthmatic response) and LAR (late asthmatic response) in a dose-dependent manner.
体外研究：
ASB14780 shows selectivity to cPLA2α (IC50 =20 nM) over type II sPLA2 (IC50 >10 μM).ASB14780 (30 min pre-incucation) inhibits cPLA2α in guinea pig whole blood (GWB) and human whole blood (HWB) in a species-derived differences, with IC50s of 0.54 μM and 0.64 μM, respectively, 15 min after being stimulated by 5 μM calcium ionophore A23187.
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备