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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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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 |
Synonyms | Ensifentrine|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 |
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Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Phosphodiesterase 3 inhibitor |
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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IUPAC Name | 2-[9,10-dimethoxy-4-oxo-2-(2,4,6-trimethylphenyl)imino-6,7-dihydropyrimido[6,1-a]isoquinolin-3-yl]ethylurea |
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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 |
PubChem CID | 9934746 |
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ChEMBL Ligand | CHEMBL4594287 |
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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] |