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ASB14780 is an indole-based selective and potent cytosolic phospholipase A2α inhibitor (IC50 = 20 nM/cPLA2α and >10 μM/sPLA2α). ASB14780 inhibits cPLA2α-dependent inflammatory responses both in cultures and in animals in vivo, including LPS-induced PGE2 production (IC50 = 0.5 μM; mouse peritoneal exudate cells), A23187-induced TXB2 production (IC50 = 0.54 and 0.64 μM 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).
| Molecular Weight | 582.69 |
| Formula | C31H27NO3 · C4H11NO3 |
| CAS Number | 1069046-00-9 |
| Solubility (25°C) | DMSO: 10 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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