Roflumilast-d₄

Roflumilast-d₄ is intended for use as an internal standard for the quantification of roflumilast (Item No. 15141) by GC- or LC-MS. Roflumilast is an inhibitor of phosphodiesterase 4 (PDE4; IC₅₀ = 0.8 nM).¹ It is selective for PDE4 over PDE1, -2, -3, and -5 (IC₅₀s = >10, >10, >10, and 8 µM, respectively). Roflumilast inhibits the production of leukotriene B₄ (LTB₄; Item No. 20110) induced by fMLP (Item No. 21495) in isolated human neutrophils with an IC₅₀ value of 2 nM. It reduces the proliferation of anti-CD3 and anti-CD28-stimulated isolated human CD4⁺ T cells (IC₃₀ = 7 nM). Roflumilast (5 mg/kg) prevents pulmonary inflammatory cell infiltration and emphysema in mice exposed to cigarette smoke.² Formulations containing roflumilast have been used in the treatment of chronic obstructive pulmonary disease (COPD).

WARNING This product is not for human or veterinary use.

1. Hatzelmann, A., and Schudt, C. Anti-inflammatory and immunomodulatory potential of the novel PDE4 inhibitor roflumilast in vitro. J. Pharmacol. Exp. Ther. 297(1), 267-279 (2001).

2. Martorana, P.A., Lunghi, B., Lucattelli, M., et al. Effect of roflumilast on inflammatory cells in the lungs of cigarette smoke-exposed mice. BMC Pulm. Med. 8, 17 (2008).