Synonyms: 3-(3-Phenethyl-1-(4-phenoxyphenyl)-1H-indol-5-yl)propanoic acid, 2-amino-2-(hydroxymethyl)-1,3-propanediol; 3-[1-(4-Phenoxyphenyl)-3-(2-phenylethyl)-1H-indol-5-yl]propanoic acid, 2-amino-2-(hydroxymethyl)-1,3-propanediol
Molecular Formula: C31H27NO3 · C4H11NO3
Molecular Weight: 582.69
Linear Structural Formula: C31H27NO3 · C4H11NO3
Purity: >=98% (HPLC)
Storage: 2-8C
Biochem Physiol Actions: ASB14780 is an indole-based selective and potent cytosolic phospholipase A2alpha inhibitor (IC50 = 20 nM/cPLA2alpha and >10 muM/sPLA2alpha). ASB14780 inhibits cPLA2alpha-dependent inflammatory responses both in cultures and in animals in vivo, including LPS-induced PGE2 production (IC50 = 0.5 muM; mouse peritoneal exudate cells), A23187-induced TXB2 production (IC50 = 0.54 and 0.64 muM using guinea pig and human whole blood, respectively), TPA-induced ear edema (50 mg/kg, p.o.; mice), OVA-induced asthma (5 - 20 mg/kg/d, p.o.; guinea pig), CCl4-induced hepatic fibrosis and high-fat cholesterol diet-induced fatty liver (0.1-0.3 g/kg/d, p.o.; mouse). SB14780 bioavailability is also demonstrated in dog and monkey, albeit at a lower value (F = 34.3%/dog and 30.9%/monkey vs. 89.6%/mouse).