E6005

E6005 is an inhibitor of phosphodiesterase 4 (PDE4, IC50 = 2.8 nM). It is selective for PDE4 over PDE1, PDE2, PDE3, and PDE5 with only 46.1, 51.6, 69.4, and 57.4% inhibition, respectively, at 30 µM. It inhibits the production of various cytokines in isolated human lymphocytes and monocytes (IC50s = 0.49-3.1 nM). Topical application of E6005 (0.003-0.3%) reduces ear thickness in a mouse model of oxazolone-induced skin inflammation, as well as reduces oxazolone-induced scratching in mice. It reduces the severity of skin lesions in a model of mite-induced atopic dermatitis. Topical application of E6005 (0.03%) also inhibits the production of leukotriene B4 (LTB4, Cay-20110) in mouse skin, as well as reduces scratching and cutaneous nerve firing induced by the proteinase-activated receptor 2 (PAR2) agonist SLIGRL-NH2 (Cay-16723) in mice.Formal Name: 4-[[[3-[6,7-dimethoxy-2-(methylamino)-4-quinazolinyl]phenyl]amino]carbonyl]-benzoic acid, methyl ester. CAS Number: 947620-48-6. Synonyms: RVT-501. Molecular Formula: C26H24N4O5. Formula Weight: 472.5. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: 1mg/mL, DMSO:PBS (pH 7.2) (1:2): 0.3mg/mL. SMILES: O=C(OC)C1=CC=C(C(NC2=CC(C3=NC(NC)=NC4=C3C=C(OC)C(OC)=C4)=CC=C2)=O)C=C1. InChi Code: InChI=1S/C26H24N4O5/c1-27-26-29-20-14-22(34-3)21(33-2)13-19(20)23(30-26)17-6-5-7-18(12-17)28-24(31)15-8-10-16(11-9-15)25(32)35-4/h5-14H,1-4H3,(H,28,31)(H,27,29,30). InChi Key: BBTFKAOFCSOZMB-UHFFFAOYSA-N.