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ASB14780

Cat. No. M8731

All AbMole products are for research use only, cannot be used for human consumption.

ASB14780 Structure

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Quality Control & Documentation
Biological Activity

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).

Chemical Information
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
References

[1] Satoshi Akiba, et al. Inhibition of Group IVA Phospholipase A 2 as a Novel Therapeutic Strategy for Nonalcoholic Steatohepatitis

[2] Shiho Kanai, et al. ASB14780, an Orally Active Inhibitor of Group IVA Phospholipase A2, Is a Pharmacotherapeutic Candidate for Nonalcoholic Fatty Liver Disease

[3] Toshiyuki Tomoo, 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

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Keywords: ASB14780 supplier, inhibitors, activators

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