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| Product Name: | E6005 | | Synonyms: | E6005;RVT-501;lotamilast;E 6005: RVT-501;METHYL 4-((3-(6,7-DIMETHOXY-2-(METHYLAMINO)QUINAZOLIN-4-YL)PHENYL)CARBAMOYL)BENZOATE;RVT-501 E6005;methyl 4-[({3-[6,7-dimethoxy-2-(methylamino)quinazolin-4-yl]phenyl}amino)carbonyl]benzoate;CS-2517 | | CAS: | 947620-48-6 | | MF: | C26H24N4O5 | | MW: | 472.49 | | EINECS: | | | Product Categories: | | | Mol File: | 947620-48-6.mol |  |
| | E6005 Chemical Properties |
| storage temp. | Store at -20°C | | solubility | DMSO:25.0(Max Conc. mg/mL);52.9(Max Conc. mM) | | form | A solid |
| | E6005 Usage And Synthesis |
| Description | 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; ) in mouse skin, as well as reduces scratching and cutaneous nerve firing induced by the proteinase-activated receptor 2 (PAR2) agonist SLIGRL-NH2 in mice. | | Uses | RVT 501 is a potent and selective inhibitor of human phosphodiesterase 4 (PDE4). |
| | E6005 Preparation Products And Raw materials |
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