| Bioactivity | ASB14780 is a 4-phenoxy derivative, the cytosolic Phospholipase A2α (cPLA2α) inhibitor, with an IC50 value of 20 nM[1]. | ||||||||||||
| Target | IC50: 20 nM (cPLA2α); 0.54 μM (guinea pig cPLA2α); 0.64 μM (human cPLA2α) | ||||||||||||
| Invitro | ASB14780 shows selectivity to cPLA2α (IC50 =20 nM) over type II sPLA2 (IC50 >10 μM)[1].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[1]. | ||||||||||||
| In Vivo | TPA (tetradecanoyl phorbol acetate) causes acute inflammation with ear, resulting in edema[1].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[1].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[1].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.)[1].Oral Bioavailabilities and Pharmacokinetic Parameters of ASB14780[1]Model | ||||||||||||
| Name | ASB14780 | ||||||||||||
| CAS | 1069046-00-9 | ||||||||||||
| Formula | C35H38N2O6 | ||||||||||||
| Molar Mass | 582.69 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Tomoo T, et al. Design, synthesis, and biological evaluation of 3-(1-Aryl-1H-indol-5-yl)propanoic acids as new indole-based cytosolic phospholipase A2α inhibitors. J Med Chem. 2014. 57(17):7244-62. |