TargetMol

Ensifentrine

Product Code:
 
TAR-T25376
Product Group:
 
Inhibitors and Activators
Supplier:
 
TargetMol
Regulatory Status:
 
RUO
Shipping:
 
cool pack
Storage:
 
-20℃
1 / 1
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CodeSizePrice
TAR-T25376-1mg1mg£103.00
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TAR-T25376-5mg5mg£148.00
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TAR-T25376-1mL1 mL * 10 mM (in DMSO)£156.00
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TAR-T25376-10mg10mg£201.00
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TAR-T25376-25mg25mg£349.00
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TAR-T25376-50mg50mg£523.00
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TAR-T25376-100mg100mg£804.00
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Further Information

Bioactivity:
Ensifentrine 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.
CAS:
1884461-72-6
Formula:
C26H31N5O4
Molecular Weight:
477.565
Pathway:
Metabolism
Purity:
0.9845
SMILES:
COc1cc2CCn3c(cc(=N/c4c(C)cc(C)cc4C)n(CCNC(N)=O)c3=O)-c2cc1OC
Target:
PDE

References

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.