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Chemical Structure : Roflumilast
CAS No.: 162401-32-3
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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 50 mg | $178 | In stock | |
| 100 mg | $288 | In stock | |
| 200 mg | $428 | In stock | |
| 1 g | Get quote |
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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.
| M.Wt | 403.21 | |
| Formula | C17H14Cl2F2N2O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
O=C(NC1=C(Cl)C=NC=C1Cl)C2=CC=C(OC(F)F)C(OCC3CC3)=C2 |
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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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