ASB14780

ASB14780

Biochem/physiol Actions

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).

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.

Packaging

5, 25 mg in glass bottle

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Code Description Colour Quality Level Manufacturer Storage Temp. Solubility Form Assay Price Quantity
3575541 ASB14780 white to beige 100 SIGMA-ALDRICH 2-8°C
£612.86 (exc VAT) per 25MG
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3575542 ASB14780 white to beige 100 SIGMA-ALDRICH 2-8°C
£151.82 (exc VAT) per 5MG
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