Roflumilast (APTA-2217) | PDE4 inhibitor

Chemical Structure : Roflumilast

CAS No.: 162401-32-3

Roflumilast (APTA-2217, BYK 20869)

Catalog No.: 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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10 mg	$58	In stock
25 mg	$98	In stock
50 mg	$148	In stock
100 mg	$238	In stock
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Biological Activity

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.

Physicochemical Properties

M.Wt	403.21
Formula	C17H14Cl2F2N2O3
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl)-4-(difluoromethoxy)benzamide

References

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.

Roflumilast (APTA-2217, BYK 20869)

Biological Activity

Physicochemical Properties

References

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