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ensifentrine , Phosphodiesterase 3 inhibitor, CAS No.E610137, Phosphodiesterase 3 inhibitor

  • Moligand™
Item Number
E610137
Grouped product items
SKUSizeAvailabilityPrice Qty
E610137-5mg
5mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$270.90
E610137-25mg
25mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$950.90

Basic Description

SynonymsEnsifentrine|RPL-554|RPL554|1884461-72-6|298680-25-8|Ensifentrine [INN]|Ensifentrine [USAN]|LS-193855|3E3D8T1GIX|LS-193,855|a]isoquinolin-3(4H)-yl}ethyl)urea|2-[9,10-dimethoxy-4-oxo-2-(2,4,6-trimethylphenyl)imino-6,7-dihydropyrimido[6,1-a]isoquinolin-3-yl
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionPhosphodiesterase 3 inhibitor

Associated Targets

PDE3A Tclin cGMP-inhibited 3',5'-cyclic phosphodiesterase A 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PDE4A Tclin cAMP-specific 3',5'-cyclic phosphodiesterase 4A 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Names and Identifiers

IUPAC Name 2-[9,10-dimethoxy-4-oxo-2-(2,4,6-trimethylphenyl)imino-6,7-dihydropyrimido[6,1-a]isoquinolin-3-yl]ethylurea
INCHI InChI=1S/C26H31N5O4/c1-15-10-16(2)24(17(3)11-15)29-23-14-20-19-13-22(35-5)21(34-4)12-18(19)6-8-30(20)26(33)31(23)9-7-28-25(27)32/h10-14H,6-9H2,1-5H3,(H3,27,28,32)
InChi Key CSOBIBXVIYAXFM-UHFFFAOYSA-N
Canonical SMILES Cc1cc(c(c(c1)C)N=c1cc2c3cc(c(cc3CCn2c(=O)n1CCNC(=O)N)OC)OC)C
Isomeric SMILES CC1=CC(=C(C(=C1)C)N=C2C=C3C4=CC(=C(C=C4CCN3C(=O)N2CCNC(=O)N)OC)OC)C
PubChem CID 9934746

Certificates

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Related Documents

References

1. Boswell-Smith V, Spina D, Oxford AW, Comer MB, Seeds EA, Page CP.  (2006)  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,  318  (2): (840-8).  [PMID:16682455]
2. Venkatasamy R, Spina D.  (2016)  Novel relaxant effects of RPL554 on guinea pig tracheal smooth muscle contractility..  Br J Pharmacol,  173  (15): (2335-51).  [PMID:27174172]
3. Turner MJ, Dauletbaev N, Lands LC, Hanrahan JW.  (2020)  The Phosphodiesterase Inhibitor Ensifentrine Reduces Production of Proinflammatory Mediators in Well Differentiated Bronchial Epithelial Cells by Inhibiting PDE4..  J Pharmacol Exp Ther,  375  (3): (414-429).  [PMID:33012706]
4. Singh D, Abbott-Banner K, Bengtsson T, Newman K.  (2018)  The short-term bronchodilator effects of the dual phosphodiesterase 3 and 4 inhibitor RPL554 in COPD..  Eur Respir J,  52  (5): (589-97).  [PMID:30166326]
5. Cazzola M, Page C.  (2018)  An inhaled "bifunctional" dual PDE3/4 inhibitor provides additional short-term improvements in lung function compared to existing classes of bronchodilator: implications for future treatment of COPD..  Eur Respir J,  52  (5): (589-97).  [PMID:30385603]
6. Bjermer L, Abbott-Banner K, Newman K.  (2019)  Efficacy and safety of a first-in-class inhaled PDE3/4 inhibitor (ensifentrine) vs salbutamol in asthma..  Pulm Pharmacol Ther,  58  (3): (101814).  [PMID:31202957]

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