Ensifentrine free base · Synonyms: RPL554

Ensifentrine is an inhaled first-in-class dual inhibitor of phosphodiesterase 3.

For research use only. Not for human or veterinary use.

Target Phosphodiesterase (PDE)

Research area Infection Neurological Disease Inflammation/Immunology Cancer

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Data Sheet SDS COA

Ensifentrine structure

CAS No.: 1884461-72-6

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
5 g	USD 1,120.00	BP-01946-5g	In stock	Get quote
10 g	Inquire	BP-01946-10g	Inquire	Inquire
25 g	Inquire	BP-01946-25g	Inquire	Inquire

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Description

Ensifentrine (RPL554) is an inhaled first-in-class dual inhibitor of phosphodiesterase 3 (PDE3) and PDE4 with IC50s of 0.4 nM and 1479 nM, respectively.

Biological activity

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.

Identifiers

SMILES: CC1=CC(C)=C(/N=C2C=C3C4=CC(OC)=C(OC)C=C4CCN3C(N\2CCNC(N)=O)=O)C(C)=C1
InChIKey: CSOBIBXVIYAXFM-BYNJWEBRSA-N

Specifications

MW (average): 477.5554
Formula: C₂₆H₃₁N₅O₄
CAS No.: 1884461-72-6
Physical state: Solid
Color: Light yellow to green yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 3 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO 5 mg/mL

Documents

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.

[3]. Anzueto A, et al. Ensifentrine, a Novel Phosphodiesterase 3 and 4 Inhibitor for the Treatment of Chronic Obstructive Pulmonary Disease: Randomized, Double-Blind, Placebo-controlled, Multicenter Phase III Trials (the ENHANCE Trials). Am J Respir Crit Care Med. 2023 Aug 15;208(4):406-416.

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