ASB14780|cas:1069046-00-9|西域试剂

ASB14780,98.0%

产品编号：Bellancom-119019| CAS NO：1069046-00-9| 分子式：C₃₅H₃₈N₂O₆| 分子量：582.69

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货号	价格	库存与货期
Bellancom-119019	￥1400.00	杭州北京（现货）
Bellancom-119019	￥2250.00	杭州北京（现货）
Bellancom-119019	￥4500.00	杭州北京（现货）

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ASB14780

产品介绍

ASB14780 是一类 4- 苯氧衍生物，是胞质磷脂酶 cPLA₂α 抑制剂，IC₅₀ 为 20 nM。

生物活性

ASB14780 is a 4-phenoxy derivative, the cytosolic Phospholipase A₂α (cPLA₂α) inhibitor, with an IC₅₀ value of 20 nM.

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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 ASB14780

Model	F (%)	AUC (h•μg/mL)	C_max (μg/mL)
mouse	89.6	7.12	5.12
dog	34.3	17.1	4.96
monkey	30.9	4.96	2.29

Note: Based on 10 mg/kg p.o. dosing data.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

Model	F (%)	AUC (h•μg/mL)	C_max (μg/mL)
mouse	89.6	7.12	5.12
dog	34.3	17.1	4.96
monkey	30.9	4.96	2.29

Note: Based on 10 mg/kg p.o. dosing data.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.