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CAS No.: 947620-48-6

Lotamilast Catalog No. CSN24782

Synonyms: RVT-501;E6005;lotamilast

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

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400-920-2911

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描述Phosphodiesterase 4 (PDE4), which catalyses the conversion of cAMP to 5′‐AMP, plays a important role in the pathogenesis of inflammatory disorders. Lotamilast, also called RVT-501/ E6005, potently and selectively inhibits human PDE4 activity with an IC50 of 2.8 nM. In mice models of atopic dermatitis, the topical application of Lotamilast produced an immediate antipruritic effect as well as an anti-inflammatory effect with reduced expression of cytokines/adhesion molecules^[1]. Topical application of 0.03% Lotamilast to the rostral back significantly inhibited the increased activity of the cutaneous nerve in mice with chronic dermatitis and this dose did not affect nerve activity evoked by punctuate stimulation with a von Frey filament^[2].
参考文献

[1] Ishii N, Shirato M, Wakita H, 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;346(1):105‐112.
[2] Andoh T, Yoshida T, Kuraishi Y. Topical E6005, a novel phosphodiesterase 4 inhibitor, attenuates spontaneous itch-related responses in mice with chronic atopy-like dermatitis. Exp Dermatol. 2014;23(5):359‐361.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1164 mL
- 10.5822 mL
- 21.1644 mL
- 5 mM
- 0.4233 mL
- 2.1164 mL
- 4.2329 mL
- 10 mM
- 0.2116 mL
- 1.0582 mL
- 2.1164 mL

技术信息

CAS号

947620-48-6

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C26H24N4O5

运输

蓝冰

分子量

472.49

别名

RVT-501;E6005;lotamilast

溶解度

DMSO	160.0 mg/mL (338.6 mM)
Water	insoluble

动物实验配方

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