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Lotamilast

CAS No. : 947620-48-6

MCE 国际站：Lotamilast

产品活性：Lotamilast (RVT-501; E6005) 是选择性的磷酸二酯酶4 (PDE4) 抑制剂，IC₅₀ 值为2.8 nM。

研究领域：Metabolic Enzyme/Protease

作用靶点：Phosphodiesterase (PDE)

In Vitro: Lotamilast potently and selectively inhibits human PDE4 activity with an IC₅₀ of 2.8 nM and suppresses the production of various cytokines from human lymphocytes and monocytes with IC₅₀ values ranging from 0.49 to 3.1 nM.

In Vivo: Lotamilast is currently in phase 2 development for patients with mild-to-moderate atopic dermatitis. In mice models, the topical application of Lotamilast produces an immediate antipruritic effect as well as an anti-inflammatory effect with reduced expression of cytokines/adhesion molecules. On the basis of these observed effects, topical RVT-501 ameliorates the appearance of atopic dermatitis-like skin lesions in two types of AD models, hapten- and mite-elicited models, exhibiting inhibitory effects comparable to that of tacrolimus. A single topical application of Lotamilast significantly inhibits spontaneous scratching during 1–2 h after application in mice with chronic dermatitis; the inhibition is partial and similar between 0.01% and 0.03%. Topical application of 0.03% Lotamilast to the rostral back significantly inhibits the increased activity of the cutaneous nerve in mice with chronic dermatitis. The cutaneous concentration of cAMP is significantly decreased in mice with chronic dermatitis, and this decrease is reversed by topical Lotamilast application.

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