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

Crisaborole (Synonyms: AN-2728; PF-06930164)

Cat. No.: HY-10978 Purity: 96.55%
Handling Instructions

Crisaborole (AN-2728) is a potent inhibitor of PDE4 and cytokine release; inhibit PDE4 with an IC50 of 0.49 μM.

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

Crisaborole Chemical Structure

Crisaborole Chemical Structure

CAS No. : 906673-24-3

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10 mM * 1 mL in DMSO USD 55 In-stock
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50 mg USD 59 In-stock
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100 mg USD 92 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

Crisaborole (AN-2728) is a potent inhibitor of PDE4 and cytokine release; inhibit PDE4 with an IC50 of 0.49 μM.

IC50 & Target

IC50: 0.49 μM (PDE4)[1]

In Vitro

Crisaborole (AN-2728) inhibits PDE4, TNF-α, IL-2, IFN-γ, IL-5 and IL-10 with IC50 values of 0.49, 0.54, 0.61, 0.83, 2.4 and 5.3 μM. Crisaborole (AN-2728) shows the most potent activity against PDE4 catalytic domain, but it also shows inhibition against PDE1A3, PDE3Cat, and PDE7A1. Crisaborole (AN-2728) inhibits PDE isozymes PDE1A3, PDE3Cat , PDE4Cat and PDE7A1 with IC50 values of 6.1, 6.4, 0.11 and 0.73 μM[1]. Crystallography reveals that interaction of benzoxaboroles with the hydrophobic pocket in the PDE4 catalytic domain increase their affinity for PDE4. These benzoxaboroles strongly suppresses the secretion of cytokines associated with Ps and AD[2]. Crisaborole (AN-2728) is a topically administered, boron-containing, anti-inflammatory compound that inhibits PDE4 activity and thereby suppresses the release of TNFalpha, IL-12, IL-23 and other cytokines[3].

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

In Vivo

Crisaborole (AN-2728) shows significant inhibition against the ear edema caused by phorbol ester after dosing at 1 mg/ear×2 (78% and 68%, respectively). The efficacy is comparable to that of dexamethasone, suggesting that Crisaborole (AN-2728) has good anti-inflammatory activity as well as skin penetration[1]. Crisaborole (AN-2728) is reported to be well tolerated and to demonstrate significant effects on markers of efficacy, with results that are comparable to positive controls in clinical trials[3].

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

Clinical Trial
Molecular Weight

251.05

Formula

C₁₄H₁₀BNO₃

CAS No.

906673-24-3

SMILES

N#CC1=CC=C(OC2=CC=C(B(O)OC3)C3=C2)C=C1

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 (398.33 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.9833 mL 19.9164 mL 39.8327 mL
5 mM 0.7967 mL 3.9833 mL 7.9665 mL
10 mM 0.3983 mL 1.9916 mL 3.9833 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: ≥ 2.5 mg/mL (9.96 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (9.96 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (9.96 mM); Clear solution

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

CrisaboroleAN-2728 PF-06930164AN2728AN 2728PF06930164PF 06930164PF-06930164Phosphodiesterase (PDE)Inhibitorinhibitorinhibit

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Crisaborole
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