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

Difamilast (Synonyms: OPA-15406)

Cat. No.: HY-109085 Purity: 99.20%
Handling Instructions

Difamilast (OPA-15406) is a topical, selective and nonsteroidal phosphodiesterase-4 (PDE4) inhibitor with particularly efficient inhibition of subtype B (IC50=11.2 nM). Difamilast can be used for the research of mild to moderate atopic dermatitis (AD).

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

Difamilast Chemical Structure

Difamilast Chemical Structure

CAS No. : 937782-05-3

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10 mM * 1 mL in DMSO Check price and availability
5 mg Check price and availability
10 mg Check price and availability
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Description

Difamilast (OPA-15406) is a topical, selective and nonsteroidal phosphodiesterase-4 (PDE4) inhibitor with particularly efficient inhibition of subtype B (IC50=11.2 nM). Difamilast can be used for the research of mild to moderate atopic dermatitis (AD)[1][2][3].

IC50 & Target[1]

PDE4B

11.2 nM (IC50)

In Vitro

OPA-15406 is highly selective for inhibition of PDE4 subtype B (IC50=11.2 nM), and OPA-15406 also exerts inhibitory effects on PDE2[2].

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

In Vivo

OPA-1540 improves skin condition in relevant animal models of AD[1].

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

Clinical Trial
Molecular Weight

446.44

Formula

C₂₃H₂₄F₂N₂O₅

CAS No.

937782-05-3

SMILES

CC(C)OC(C=C(C1=NC(CNC(C(C=CC=C2)=C2OCC)=O)=CO1)C=C3)=C3OC(F)F

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 : 100 mg/mL (223.99 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2399 mL 11.1997 mL 22.3994 mL
5 mM 0.4480 mL 2.2399 mL 4.4799 mL
10 mM 0.2240 mL 1.1200 mL 2.2399 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: 2.5 mg/mL (5.60 mM); Suspended solution; Need ultrasonic

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.60 mM); Clear solution

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

DifamilastOPA-15406OPA15406OPA 15406Phosphodiesterase (PDE)phosphodiesterase-4PDE4subtypeBatopicdermatitisADInhibitorinhibitorinhibit

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