产品描述:
Pamapimod is a potent inhibitor of p38α MAP kinase (IC50 = 14 nM).{33190} It displays over 30-fold selectivity for p38α over p38β, has no activity against p38δ or p38γ, and has limited activity against a panel of 350 other kinases. Pamapimod blocks LPS-induced TNF-α production by monocytes and IL-1β generation in whole blood, and it inhibits spontaneous TNF-α release from synovial explants from patients with rheumatoid arthritis.{33191,33189} It is orally bioavailable and abrogates inflammation and bone loss in an animal model of arthritis and pain in a rat model of hyperalgesia.{33191} Pamapimod suppresses the expression of inflammation-associated genes in primary, IL-1β-stimulated human chondrocytes.{33192}