Ensifentrine tosylate  (Synonyms: RPL-554 tosylate)

Ensifentrine (RPL-554) tosylate is an inhaled dual inhibitor of PDE3 and PDE4 with IC₅₀s of 0.4 nM and 1479 nM, respectively. Ensifentrine tosylate blocks PDE3 and PDE4 enzymes, thereby increasing the levels of cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) in lung cells, dilating the bronchi, and inhibiting the activation and migration of inflammatory cells. Ensifentrine tosylate can be used in the research of chronic obstructive pulmonary disease (COPD)^[1][2][3].

649.76

C₃₃H₃₉N₅O₇S

3098314-20-3

O=S(O)(C1=CC=C(C=C1)C)=O.O=C2N3C(C4=CC(OC)=C(OC)C=C4CC3)=C/C(N2CCNC(N)=O)=N\C5=C(C=C(C=C5C)C)C

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Victoria Boswell-Smith, et al. The pharmacology of two novel long-acting phosphodiesterase 3/4 inhibitors, RPL554 [9,10-dimethoxy-2(2,4,6-trimethylphenylimino)-3-(n-carbamoyl-2-aminoethyl)-3,4,6,7-tetrahydro-2H-pyrimido[6,1-a]isoquinolin-4-one] and RPL565 [6,7-dihydro-2-(2,6-diisopropylphenoxy)-9,10-dimethoxy-4H-pyrimido[6,1-a]isoquinolin-4-one]. J Pharmacol Exp Ther. 2006 Aug;318(2):840-8.  [Content Brief]

  [2]. Henrik Watz, et al. Symptom Improvement Following Treatment with the Inhaled Dual Phosphodiesterase 3 and 4 Inhibitor Ensifentrine in Patients with Moderate to Severe COPD - A Detailed Analysis. Int J Chron Obstruct Pulmon Dis. 2020 Sep 16;15:2199-2206.  [Content Brief]

  [3]. Anzueto A, et al. Ensifentrine, a Novel Phosphodiesterase 3 and 4 Inhibitor for the Treatment of Chronic Obstructive Pulmonary Disease: Randomized, Double-Blind, Placebo-controlled, Multicenter Phase III Trials (the ENHANCE Trials). Am J Respir Crit Care Med. 2023 Aug 15;208(4):406-416.  [Content Brief]