Ensifentrine
Ensifentrine Basic information
- Product Name:
- Ensifentrine
- Synonyms:
-
- Urea, N-[2-[(2E)-6,7-dihydro-9,10-dimethoxy-4-oxo-2-[(2,4,6-trimethylphenyl)imino]-2H-pyrimido[6,1-a]isoquinolin-3(4H)-yl]ethyl]-
- Ensifentrine
- Ensifentrine ( RPL554 )
- EnsifentrineQ: What is Ensifentrine Q: What is the CAS Number of Ensifentrine
- Ensifentrina
- Ensifentrinum
- RPL 554,RPL554,inhaled,Inhibitor,RPL-554,Ensifentrine,bronchoprotective,inhibit,COPD,PDE4,anti-inflammatory,PDE3,Phosphodiesterase (PDE)
- Ensifentrine, 10 mM in DMSO
- CAS:
- 1884461-72-6
- MF:
- C26H31N5O4
- MW:
- 477.56
- Product Categories:
-
- APIS
- Mol File:
- 1884461-72-6.mol
Ensifentrine Chemical Properties
- Density
- 1.29±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO : 25 mg/mL (52.35 mM; Need ultrasonic)
- form
- Solid
- pka
- 13.73±0.46(Predicted)
- color
- Light yellow to green yellow
- InChIKey
- CSOBIBXVIYAXFM-BYNJWEBRSA-N
- SMILES
- N(CCN1/C(=N/C2=C(C)C=C(C)C=C2C)/C=C2C3=C(C=C(OC)C(OC)=C3)CCN2C1=O)C(N)=O
Ensifentrine Usage And Synthesis
Uses
RPL 554 is a known drug candidate for respiratory diseases, particularly in patients with asthma or chronic obstructive pulmonary diseases.
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. |
IC 50
PDE3: 0.4 nM (IC50); PDE4: 1479 nM (IC50)
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