货号	规格	价格	上海	北京	珠海	重庆	武汉
S87496-5mg买3赠1	≥98%	￥240.00 S87496-5mg ￥240.00 2-3天（买3赠1）	0 货期：2-3天	-	-	-	-
S87496-10mg买3赠1	98.30%	￥320.00 S87496-10mg ￥320.00 现货（买3赠1）	3 3	-	-	-	-
S87496-50mg	98.30%	￥970.00 S87496-50mg ￥970.00 现货	5 5	-	-	-	-
S87496-100mg	98.30%	￥1740.00 S87496-100mg ￥1740.00 现货	6 6	-	-	-	-

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产品描述：

Lotamilast (RVT-501; E6005) is a selective phosphodiesterase 4 (PDE4) inhibitor with an IC50 of 2.8 nM.

靶点：

IC50: 2.8 nM (human PDE4);PDE

体外研究：

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

体内研究：

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

参考文献：

1. Ishii N, et al. Antipruritic effect of the topical phosphodiesterase 4 inhibitor E6005 ameliorates skin lesions in a mouse atopic dermatitis model. J Pharmacol Exp Ther. 2013 Jul;346(1):105-12. 2. Andoh T, et al. Topical E6005, a novel phosphodiesterase 4 inhibitor, attenuates spontaneous itch-related responses in mice with chronic atopy-like dermatitis. Exp Dermatol. 2014 May;23(5):359-61.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.116 ml	10.582 ml	21.164 ml
5 mM	0.423 ml	2.116 ml	4.233 ml
10 mM	0.212 ml	1.058 ml	2.116 ml
50 mM	0.042 ml	0.212 ml	0.423 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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