(E/Z)-Ensifentrine
(E/Z)-Ensifentrine ((E/Z)-RPL-554) is the E/Z isomer of Ensifentrine (HY-119708). Ensifentrine is an inhaled dual PDE3 and PDE4 inhibitor. Ensifentrine can be used in research on chronic obstructive pulmonary disease (COPD).
For research use only. We do not sell to patients.
- CAS No.: 298680-25-8
- Formula: C26H31N5O4
- Molecular Weight:477.56
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
PDE4 |
PDE3 |
In Vitro
Ensifentrine is a PDE3/4 inhibitor that exhibits broad bronchodilatory and anti-inflammatory activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 298680-25-8
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Molecular Weight 477.56
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Formula C26H31N5O4
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SMILES
O=C(N)NCCN1C(N(CCC2=C3C=C(OC)C(OC)=C2)C3=C/C1=N\C4=C(C)C=C(C)C=C4C)=O
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Synonyms
(E/Z)-RPL-554
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)