Ensifentrine

Modify Date: 2024-01-05 06:11:24

Ensifentrine structure	Common Name	Ensifentrine
	CAS Number	1884461-72-6	Molecular Weight	477.56
	Density	N/A	Boiling Point	N/A
	Molecular Formula	C26H31N5O4	Melting Point	N/A
	MSDS	N/A	Flash Point	N/A

Purity		Quantity		Budget		Inquiry

Use of Ensifentrine Ensifentrine (RPL-554) is an inhaled first-in-class dual inhibitor of phosphodiesterase 3 (PDE3) and PDE4 with IC50s 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[1][2].

• Properties

• Spectrum

---

 Names

Name	Ensifentrine

 Ensifentrine Biological Activity

Description	Ensifentrine (RPL-554) is an inhaled first-in-class dual inhibitor of phosphodiesterase 3 (PDE3) and PDE4 with IC50s 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[1][2].
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphodiesterase (PDE) Research Areas >> Inflammation/Immunology
Target	PDE3:0.4 nM (IC50) PDE4:1479 nM (IC50)
In Vitro	Ensifentrine (RPL-554) inhibits, in a concentration-dependent manner, lipopolysaccharide-induced TNF-α release from human monocytes (IC50 of 0.52 μM) and proliferation of human mononuclear cells to phytohemagglutinin (IC50 of 0.46 μM)[1]. 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[1].
In Vivo	Ensifentrine (RPL-554; 10 mg/kg; Oral administration; once) significantly inhibits eosinophil recruitment following antigen challenge in ovalbumin-sensitized guinea pigs[1]. 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[1]. 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[1]. Animal Model: Male Dunkin Hartley guinea pigs (200-300 g) injected with ovalbumin[1]. Dosage: 10 mg/kg Administration: Oral administration; once Result: Significantly inhibits eosinophil recruitment following antigen challenge in ovalbumin-sensitized guinea pigs.
References	[1]. 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. [2]. 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.

 Chemical & Physical Properties

Molecular Formula	C26H31N5O4
Molecular Weight	477.56

Company Profile

     Our company is a high-tech enterprise specializing in chemical raw materials such as electronic materials, optoelectronic materials, semiconductor materials, UV monomers, silane catalysts, cosmetic raw materials, etc. 

     We are committed to providing high-quality chemical products and comprehensive solutions to meet the diverse needs of the global market.

     Our research and development team possesses profound professional knowledge and extensive industry experience, dedicated to developing cutting-edge chemical materials to drive technological progress and industrial development. Our production facilities are equipped with state-of-the-art technology and a stringent quality control system to ensure product consistency and reliability.

     As a pioneer in the industry, we not only offer standardized products but also customize chemicals and services according to the specific needs of our customers. Our goal is to become a trusted partner for global customers through continuous technological innovation and superior customer service.

Our Company

Our Advantage

Quality control

Based on industry norms, customer requirements, and internal quality objectives, we establish clear quality standards. By monitoring the production process in real-time, we ensure that every step conforms to the predetermined quality standards.

Excellent quality is one of the cornerstones of our success. We welcome ordering samples for quality testing.

Technological innovation

Our technological innovation is reflected in the development of new materials that are at the leading edge of the industry. These materials not only possess higher performance and lower costs but also enable sustainable use within an environmentally friendly production process.

Competitiveness

Based on rich experience in material development and production, we have established a more scientific cost control system. By ensuring product quality, and through refined management and continuous process optimization, we offer more competitive prices.

Word of mouth

Adhering to the principle of customer first, customer first, and honest service, we have established long-term business relationships with customers and are deeply welcomed and trusted by them.

Rich experience

Our products have been exported to many countries, including Germany, Spain, the United Kingdom, the United States, Australia, the Middle East, Asia, and more. We have received highly positive feedback from our clients and have established long-term friendly cooperative relationships with them.

Safe and fast delivery

We will arrange shipment of spot products as soon as we receive payment.

Customized products are determined based on the synthesis time of different products.

Excellent pre-sales and after-sales service

Pre sales:

We are committed to providing the most favorable quotes and detailed information about our products and company.

after-sale service:

We assist buyers in customs clearance by providing necessary documents and information.

If there is any dispute over product quality, we are committed to providing the best solution.

? Packaging: 

1kg/bag, 25kg/drum, 50kg/drum, 180kg/drum, 200kg/drum, 1T/bag/drum, standard export packaging or packaging required by customers

? Shipping

? Delivery:

Within 7 days after receiving your payment

Contact information

For more details, pls contact us freely.

Contact name: Jessica

Email address : jessica@fdachem.com

Mob: 86 13676922317

WhatsApp/Skype/Wechat/LINE: 86 13676922317