SD-06

p38αMAPK抑制剂(IC50=0.016µM)；对p38α的选择性优于p38β、p38γ和p38δMAPK（IC50s分别为0.677、>100和>100µM），以及一组54种额外的激酶（所有IC50s=>3µM）；抑制LPS诱导的原代人单核细胞释放TNF-α、IL-6和IL-1β（IC50s分别为79.4、106.9和105.9nM）；降低IL-1β诱导的患者来源的RASF中PGE2的产生（IC50=96.2nM）；在30mg/kg剂量下可减轻角叉菜胶诱导的大鼠爪肿胀和痛觉过敏；降低胶原诱导性关节炎小鼠模型中关节炎的发病率；防止链球菌细胞壁诱导性关节炎大鼠模型中关节和骨骼的破坏。An inhibitor of p38α MAPK (IC50 = 0.016 µM); selective for p38α over p38β, p38γ, and p38δ MAPKs (IC50s = 0.677, >100, and >100 µM, respectively), as well as a panel of 54 additional kinases (IC50s = >3 µM for all); inhibits LPS-induced TNF-α, IL-6, and IL-1β release from primary human monocytes (IC50s = 79.4, 106.9, and 105.9 nM, respectively); decreases IL-1β-induced production of PGE2 in patient-derived RASFs (IC50 = 96.2 nM); reduces carrageenan-induced paw swelling and hyperalgesia in rats at 30 mg/kg; reduces the incidence of arthritis in a mouse model of collagen-induced arthritis; protects against joint and bone destruction in a rat model of streptococcal cell wall-induced arthritis.分子式C20H20ClN5O2分子量397.9O=C(CO)N(CC1)CCC1C2=NNC(C3=CC=C(Cl)C=C3)=C2C4=NC=NC=C4O=C(CO)N(CC1)CCC1C2=NNC(C3=CC=C(Cl)C=C3)=C2C4=NC=NC=C4