E6005

产品编号: DC10141 Featured
E6005
结构式
947620-48-6
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中国地区超过5000个高品质化合物库存
应用领域
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。
Cas No.: 947620-48-6
名称: (methyl 4-[({3-[6,7-dimethoxy-2(methylamino)quinazolin-4yl]phenyl}amino)carbonyl]benzoate
别名: E 6005,E-6005
SMILES: C1=C(OC)C(OC)=CC2N=C(NC)N=C(C3=CC(NC(C4=CC=C(C(OC)=O)C=C4)=O)=CC=C3)C1=2
分子式: C26H24N4O5
分子量: 472.49
纯度:
保存条件: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description:
In Vivo:
In Vitro:
References: E6005 potently and selectively inhibited human PDE4 activity with an IC50 of 2.8 nM and suppressed the production of various cytokines from human lymphocytes and monocytes with IC50 values ranging from 0.49 to 3.1 nM. In mice models, the topical application of E6005 produced 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 E6005 ameliorated 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. The use of 14Clabeled E6005 showed rapid clearance from the blood and low distribution to the brain, contributing to the low emetic potential of this compound. E6005 is a novel therapeutic agent with antipruritic activity for the treatment of AD.
Kinase Assay:
Cell Assay:
Animal Administration:
References:
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
产品编号 产品名称 应用领域
DC7815 Crisaborole(AN-2728) Crisaborole (AN-2728) 是有效地PDE4和cytokine释放抑制剂,抑制PDE4的 IC50 值为0.49 μM。
DC10141 E6005 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。