Ensifentrine - 10mM in DMSO , CAS No.1884461-72-6

CAS: 1884461-72-6 Cat. No.: E655682 Molecular Weight: 477.56 EC Number: 973-852-2 PubChem CID: 9934746

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Ensifentrine (RPL-554) is an inhaled first-in-class dual inhibitor of phosphodiesterase 3 (PDE3) and PDE4 with IC 50 s 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

In Vitro

Ensifentrine (RPL-554) inhibits, in a concentration-dependent manner, lipopolysaccharide-induced TNF-α release from human monocytes (IC 50 of 0.52 μM) and proliferation of human mononuclear cells to phytohemagglutinin (IC 50 of 0.46 μM). Electrical field stimulation-induced contraction of guinea pig superfused isolated tracheal preparations is significantly inhibited by Ensifentrine (10 μM). Contractile responses are suppressed for up to 12 h after termination of superfusion with RPL-554 demonstrating a long duration of action. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Ensifentrine (RPL-554; 10 mg/kg; Oral administration; once) significantly inhibits eosinophil recruitment following antigen challenge in ovalbumin-sensitized guinea pigs . The inhalation of dry powder containing Ensifentrine by conscious guinea pigs (25% in micronized lactose) 1.5 h before antigen exposure significantly inhibits the recruitment of eosinophils to the airways . Exposure of conscious guinea pigs to inhalation of dry powder containing Ensifentrine (2.5%) in micronized lactose significantly inhibits histamine-induced plasma protein extravasation in the trachea and histamine-induced bronchoconstriction over a 5.5-h period . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male Dunkin Hartley guinea pigs (200-300 g) injected with ovalbumin . Dosage: 10 mg/kg Administration: Oral administration; once Result: Significantly inhibits eosinophil recruitment following antigen challenge in ovalbumin-sensitized guinea pigs.

IC50& Target:PDE3 0.4 nM (IC 50 ) PDE4 1479 nM (IC 50 )

Specifications

Specifications & Purity

10mM in DMSO

Biochemical and Physiological Mechanisms

Ensifentrine (RPL-554) is an inhaled first-in-class dual inhibitor of phosphodiesterase 3 (PDE3) and PDE4 with IC 50 s of 0.4 nM and 1479 nM, respectively. Ensifentrine has bronchoprotective and anti-inflammatory activities. Ensifentrine can be used for c

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Action Type

INHIBITOR

Names and Identifiers

• Isomeric SMILES: CC1=CC(=C(C(=C1)C)N=C2C=C3C4=CC(=C(C=C4CCN3C(=O)N2CCNC(=O)N)OC)OC)C
• Alternate CAS: 1884461-72-6,298680-25-8
• PubChem CID: 9934746
• MeSH Entry Terms: 9,10-dimethoxy-2-(2,4,6-trimethylphenylimino)-3-(N-carbamoyl-2-aminoethyl)-3,4,6,7-tetrahydro-2H-pyrimidino(6,1-a)isoquinolin-4-one;ensifentrine;RPL 554;RPL-554;RPL554
• Molecular Weight: 477.56