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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Phosphodiesterase (PDE)-Roflumilast
Roflumilast

Chemical Structure : Roflumilast

CAS No.: 162401-32-3

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Roflumilast (APTA-2217, BYK 20869)

货号: PC-20681Not For Human Use, Lab Use Only.

Roflumilast (APTA-2217) is a potent, selective, orally active PDE4 inhibitor with IC50 of 0.7, 0.9, 0.7, and 0.2 nM for PDE4A1, PDEA4, PDEB1, and PDEB2, respectively.

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25 mg ￥980 In stock
50 mg ￥1480 In stock
100 mg ￥2380 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Roflumilast (APTA-2217) is a potent, selective, orally active PDE4 inhibitor with IC50 of 0.7, 0.9, 0.7, and 0.2 nM for PDE4A1, PDEA4, PDEB1, and PDEB2, respectively.
Roflumilast shows no PDE4 subtype selectivity apart from PDE4C (4C1, IC50=3 nM; 4C2, IC50=4.3 nM), does not inhibits PDE1, PDE2, PDE3 or PDE5 isoenzymes.
Roflumilast inhibits human neutrophil functions, inhibits TNFα synthesis in monocyte-derived dendritic cells.
Rolfumilast inhibits proliferation and cytokine synthesis in CD4+ T cells.
Roflumilast inhibits the ovalbumin-evoked contractions of tracheal chains prepared from sensitized guinea pigs with EC50 of 0.2 uM.
Roflumilast abrogated LPS-induced circulating TNFalpha in the rat (ED(50) = 0.3 micromol/kg) in bronchoalveolar lavage fluid of Brown Norway rats.

物理化学性质&存储条件

分子量 403.21
分子式 C17H14Cl2F2N2O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl)-4-(difluoromethoxy)benzamide

参考文献

1. Bundschuh DS, et al. J Pharmacol Exp Ther. 2001 Apr;297(1):280-90.

2. Hatzelmann A, et al. J Pharmacol Exp Ther. 2001 Apr;297(1):267-79.

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