A1480LS is a peripherally restricted, orally active covalent and irreversible inhibitor of DAGLalpha and DAGLbeta, with IC50 values of 6 nM and 4 nM against human targets, respectively, and IC50 values 15 nM across mouse, rat, dog, monkey and human systems. A1480LS reduces the levels of 2-arachidonoylglycerol, arachidonic acid, and cyclooxygenase- and lipoxygenase-derived eicosanoids. A1480LS inhibits injury-induced production of 2-arachidonoylglycerol and arachidonic acid in the peripheral sciatic nerve, and suppresses the responses of high-threshold and wide-dynamic-range-like dorsal horn neurons to mechanical stimulation. A1480LS alleviates pain behaviors in rat models of inflammatory pain, neuropathic pain and chemotherapy-induced peripheral neuropathy[1].
Molecular Weight:
542.55
Formula:
C30H25F3N6O
Target:
DAGL
Application Notes:
MCE Product type: Reference compound
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