Ensifentrine

Ensifentrine (RPL-554) is an inhaled dual inhibitor of PDE3 and PDE4 with IC50s of 0.4 nM and 1479 nM, respectively. Ensifentrine 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 can be used in the research of chronic obstructive pulmonary disease (COPD) [1][2][3].

Product Specifications

CAS Number

[1884461-72-6]

Product Name Alternative

RPL-554

UNSPSC

12352005

Target

Phosphodiesterase (PDE)

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

COVID-19-immunoregulation

Field of Research

Cancer; Infection; Inflammation/Immunology; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/ensifentrine.html

Purity

99.70

Solubility

DMSO : 25 mg/mL (ultrasonic)

Smiles

O=C(NCCN1C(N(C2=C/C1=N\C3=C(C=C(C=C3C)C)C)CCC4=C2C=C(C(OC)=C4)OC)=O)N

Molecular Formula

C26H31N5O4

Molecular Weight

477.56

References & Citations

[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.|[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.|[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.