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.
Shipping Conditions
Room temperature
Scientific Category
Isotope-Labeled Compounds
Clinical Information
No Development Reported
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