1. Metabolic Enzyme/Protease
  2. Phosphodiesterase (PDE)
  3. Ensifentrine

Ensifentrine (Synonyms: RPL-554)

Cat. No.: HY-119708 Purity: 99.47%
Handling Instructions

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.

For research use only. We do not sell to patients.

Ensifentrine Chemical Structure

Ensifentrine Chemical Structure

CAS No. : 1884461-72-6

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 420 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 420 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 400 In-stock
Estimated Time of Arrival: December 31
10 mg USD 680 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1350 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2200 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3400 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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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].

IC50 & Target[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

477.56

Formula

C₂₆H₃₁N₅O₄

CAS No.
SMILES

O=C(NCCN1C(N(C2=C/C1=N\C3=C(C=C(C=C3C)C)C)CCC4=C2C=C(C(OC)=C4)OC)=O)N

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (52.35 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0940 mL 10.4699 mL 20.9398 mL
5 mM 0.4188 mL 2.0940 mL 4.1880 mL
10 mM 0.2094 mL 1.0470 mL 2.0940 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1.25 mg/mL (2.62 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 1.25 mg/mL (2.62 mM); Suspended solution; Need ultrasonic

*All of the co-solvents are provided by MCE.
References
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Keywords:

EnsifentrineRPL-554RPL554RPL 554Phosphodiesterase (PDE)PDE3PDE4inhaledbronchoprotectiveanti-inflammatoryCOPDInhibitorinhibitorinhibit

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Product Name:
Ensifentrine
Cat. No.:
HY-119708
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