ASB14780

C₃₁H₂₇NO₃ · C₄H₁₁NO₃

582.69

NA.77

ASB14780 can be a potential therapeutic for the treatment of asthma and other pulmonary diseases. In addition, its inhibitory function on group IVA phospholipase A2 (IVA-PLA2) qualifies this drug to be a potential candidate for the treatment of non-alcoholic fatty liver diseases.
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).

100

≥98% (HPLC)

powder

white to beige

DMSO: 10 mg/mL, clear

2-8℃

O=C(O)CCC1=CC2=C(N(C3=CC=C(OC4=CC=CC=C4)C=C3)C=C2CCC5=CC=CC=C5)C=C1.NC(CO)(CO)CO

5, 25 mg in glass bottle

13 - Non Combustible Solids

WGK 3