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Ensifentrine

Catalog No. T25376 CAS 1884461-72-6

Synonyms: Ensifentrina, Ensifentrinum

Ensifentrine (Ensifentrinum) is a PDE3/4 inhibitor, although its affinity for PDE3(IC50: 0.4 nM) is 3,440 times higher than that for PDE4(IC50: 1479 nM), that is under clinical development for the treatment of asthma and COPD and, potentially, cystic fibrosis.

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Ensifentrine, CAS 1884461-72-6

Pack Size	Availability	Price/USD
1 mg	In stock	$ 41.00
5 mg	In stock	$ 97.00
10 mg	In stock	$ 163.00
25 mg	In stock	$ 347.00
50 mg	In stock	$ 563.00
100 mg	In stock	$ 913.00
1 mL * 10 mM (in DMSO)	In stock	$ 107.00

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Purity: 98.45%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Ensifentrine (Ensifentrinum) is a PDE3/4 inhibitor, although its affinity for PDE3(IC50: 0.4 nM) is 3,440 times higher than that for PDE4(IC50: 1479 nM), that is under clinical development for the treatment of asthma and COPD and, potentially, cystic fibrosis.
Targets&IC50	PDE3:0.4 nM, PDE4:1479 nM
In vitro	Electrical field stimulation-induced contraction of guinea pig superfused isolated tracheal preparations was significantly inhibited by Ensifentrine (10 microM) (percentage control; 93 +/- 1.2). Contractile responses were suppressed for up to 12 h after termination of superfusion with Ensifentrine demonstrating a long duration of action. Ensifentrine4 inhibited, in a concentration-dependent manner, lipopolysaccharide-induced tumor necrosis factor alpha release from human monocytes [IC50; 0.52 microM (0.38-0.69)] and proliferation of human mononuclear cells to phytohemagglutinin [IC50; 0.46 microM (0.24-0.9)][2].
In vivo	Ensifentrine administered orally significantly inhibited eosinophil recruitment following antigen challenge in ovalbumin-sensitized guinea pigs. Likewise, inhalation of dry powder containing Ensifentrine by conscious guinea pigs (25% in micronized lactose) 1.5 h before antigen exposure significantly inhibited the recruitment of eosinophils to the airways. Exposure of conscious guinea pigs to inhalation of dry powder containing Ensifentrine (2.5%) and RPL565 (25%) in micronized lactose significantly inhibited histamine-induced plasma protein extravasation in the trachea and histamine-induced bronchoconstriction over a 5.5-h period[2].

Synonyms	Ensifentrina, Ensifentrinum
Molecular Weight	477.56
Formula	C26H31N5O4
CAS No.	1884461-72-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 20 mg/ml(41.88 mM)

References and Literature

1. 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. 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. Cazzola M, et al. Ensifentrine (RPL554): an investigational PDE3/4 inhibitor for the treatment of COPD. Expert Opin Investig Drugs. 2019 Oct;28(10):827-833.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Neurodegenerative Disease Compound Library Drug Repurposing Compound Library Inhibitor Library Anti-Alzheimer's Disease Compound Library Orally Active Compound Library Bioactive Compounds Library Max Cuproptosis Compound Library Clinical Compound Library Bioactive Compound Library Metabolism Compound Library

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Keywords

Ensifentrine 1884461-72-6 Metabolism PDE RPL 554 RPL554 inhaled Inhibitor RPL-554 bronchoprotective inhibit COPD PDE4 Ensifentrina anti-inflammatory Ensifentrinum PDE3 Phosphodiesterase (PDE) inhibitor

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