ASB14780

• CAT Number: I022502
• CAS Number: 1069046-00-9
• Purity: ≥95%
• Synonyms: 2-amino-2-(hydroxymethyl)propane-1,3-diol;3-[1-(4-phenoxyphenyl)-3-(2-phenylethyl)indol-5-yl]propanoic acid
• InChI: InChI=1S/C31H27NO3.C4H11NO3/c33-31(34)20-13-24-12-19-30-29(21-24)25(14-11-23-7-3-1-4-8-23)22-32(30)26-15-17-28(18-16-26)35-27-9-5-2-6-10-27;5-4(1-6,2-7)3-8/h1-10,12,15-19,21-22H,11,13-14,20H2,(H,33,34);6-8H,1-3,5H2
• InChIKey: MBPXGBINIINSEU-UHFFFAOYSA-N
• SMILES: C1=CC=C(C=C1)CCC2=CN(C3=C2C=C(C=C3)CCC(=O)O)C4=CC=C(C=C4)OC5=CC=CC=C5.C(C(CO)(CO)N)O

ASB14780 is a 4-phenoxy derivative, the cytosolic Phospholipase A2α (cPLA2α) inhibitor, with an IC50 value of 20 nM[1].
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].
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
F (%)
AUC (h•μg/mL)
Cmax (μg/mL)

mouse
89.6
7.12
5.12

dog
34.3
17.1
4.96