Ensifentrine

Ensifentrine is a phosphodiesterase 3 (PDE3) inhibitor (IC50 = 0.4 nM). It is selective for PDE3 over PDE4 (IC50 = 1,479 nM). Ensifentrine reduces phytohemagglutinin-induced proliferation of isolated human monocytes in a concentration-dependent manner and inhibits LPS-induced increases of TNF-alpha protein levels in isolated human monocytes (IC50 = 520 nM). It increases cAMP levels in isolated human neutrophils when used at a concentration of 10 µM. Ensifentrine inhibits electric field stimulation-induced contractile responses in isolated guinea pig trachea in a concentration-dependent manner. Intranasal administration of ensifentrine (25% w/w) inhibits histamine-induced bronchoconstriction and tracheal edema in guinea pigs.Formal Name: N-[2-[(2E)-6,7-dihydro-9,10-dimethoxy-4-oxo-2-[(2,4,6-trimethylphenyl)imino]-2H-pyrimido[6,1-a]isoquinolin-3(4H)-yl]ethyl]-urea. CAS Number: 1884461-72-6. Synonyms: RPL 554, VMX 554. Molecular Formula: C26H31N5O4. Formula Weight: 477.6. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: DMF: Slightly soluble, DMSO: Slightly soluble. lambdamax: 229, 334 nm. SMILES: O=C(N/1CCNC(N)=O)N(CC2)C(C(C2=C3)=CC(OC)=C3OC)=CC1=N/C(C(C)=CC(C)=C4)=C4C. InChi Code: 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)/b29-23+. InChi Key: CSOBIBXVIYAXFM-BYNJWEBRSA-N.