Ensifentrine-d6

Ensifentrine-d6 (RPL-554-d6) is deuterium labeled Ensifentrine. Ensifentrine (RPL-554) is an inhaled first-in-class dual inhibitor of phosphodiesterase 3 (PDE3) and PDE4 with IC50s of 0.4 nM and 1479 nM, respectively. Ensifentrine has bronchoprotective and anti-inflammatory activities. Ensifentrine can be used for chronic obstructive pulmonary disease (COPD) research[1][2].

Product Specifications

Product Name Alternative

RPL-554-d6

UNSPSC

12352005

Target

Isotope-Labeled Compounds; Phosphodiesterase (PDE)

Related Pathways

Metabolic Enzyme/Protease; Others

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Smiles

O=C1N2C(C3=CC(OC([2H])([2H])[2H])=C(OC([2H])([2H])[2H])C=C3CC2)=C/C(N1CCNC(N)=O)=N\C4=C(C=C(C=C4C)C)C

Molecular Formula

C26H25D6N5O4

Molecular Weight

483.59

References & Citations

[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-216.|[2]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.|[3]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.