An inhibitor of PDE4 (IC50 = 2.8 nM); selective for PDE4 over PDE1

E6005 – 25 mg

Brand:
Cayman
CAS:
947620-48-6
Storage:
-20
UN-No:
Non-Hazardous - /

E6005 is an inhibitor of phosphodiesterase 4 (PDE4; IC50 = 2.8 nM).{53585} 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; Item No. 20110) in mouse skin, as well as reduces scratching and cutaneous nerve firing induced by the proteinase-activated receptor 2 (PAR2) agonist SLIGRL-NH2 (Item No. 16723) in mice.{53586}  

 

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SKU: 30203 - 25 mg Category:

Description

An inhibitor of PDE4 (IC50 = 2.8 nM); 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; inhibits cytokine production in isolated human lymphocytes and monocytes (IC50s = 0.49-3.1 nM); reduces ear thickness in a mouse model of oxazolone-induced skin inflammation at 0.003-0.3%; reduces oxazolone-induced scratching in mice at 0.003-0.3%; reduces the severity of skin lesions in a model of mite-induced atopic dermatitis; inhibits LTB4 production in mouse skin, as well as reduces scratching and cutaneous nerve firing induced by SLIGRL-NH2 in mice

Formal name: 4-[[[3-[6,7-dimethoxy-2-(methylamino)-4-quinazolinyl]phenyl]amino]carbonyl]-benzoic acid, methyl ester

Synonyms:  RVT-501

Molecular weight: 472.5

CAS: 947620-48-6

Purity: ≥98%

Formulation: A solid

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