MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

Lotamilast

CAS No. : 947620-48-6

MCE 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.

相关产品：Drug Repurposing Compound Library Plus  |  Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  Immunology/Inflammation Compound Library  |  Metabolism/Protease Compound Library  |  Clinical Compound Library  |  Drug Repurposing Compound Library  |  Anti-Alzheimer’s Disease Compound Library  |  IBMX  |  Bucladesine sodium  |  Rolipram  |  Sildenafil  |  Theophylline  |  Icariin  |  Roflumilast  |  Tadalafil  |  PF-04957325  |  Milri  |  Dipyridamole  |  Pentoxifylline  |  Cilostazol  |  Ibudilast  |  Butein  |  Cilomilast  |  Cilostamide  |  EHNA hydrochloride  |  Zardaverine  |  Vardenafil hydrochloride  |  Vinpocetine  |  W-7 hydrochloride  |  BRL-50481  |  HA130  |  Aminophylline  |  Pimobendan  |  Anagrelide hydrochloride  |  Bay 60-7550

品牌介绍:
•   MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供*新*全的高品质小分子活性化合物；
•   10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种期刊及制药收录了MCE客户的科研成果；
•   专业团队跟踪*新的制药及生命科学研究进展，为您提供全球*新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。