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Crisaborole

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COA HPLC HNMR

Crisaborole

Catalog No. T4285Cas No. 906673-24-3

Crisaborole (AN-2728) is a Phosphodiesterase 4 Inhibitor.

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Pack Size	Price	Availability
10 mg	$38	In Stock
50 mg	$50	In Stock
100 mg	$83	In Stock
200 mg	$111	In Stock
1 mL x 10 mM (in DMSO)	$46	In Stock

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Product Introduction

Bioactivity

Description	Crisaborole (AN-2728) is a Phosphodiesterase 4 Inhibitor.
In vitro	AN-2728 inhibits PDE isozymes PDE1A3, PDE3Cat , PDE4Cat and PDE7A1 with IC50 values of 6.1, 6.4, 0.11 and 0.73 μM. 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. AN-2728 shows the most potent activity against PDE4 catalytic domain, but it also shows inhibition against PDE1A3, PDE3Cat, and PDE7A1. 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.
In vivo	AN-2728 is well tolerated and significantly impacts efficacy markers, showing comparable results to positive controls in clinical trials. It effectively inhibits ear edema induced by phorbol ester with a dosing of 1 mg/ear×2 (78% and 68%, respectively), mirroring the efficacy of dexamethasone. This suggests AN-2728 possesses notable anti-inflammatory properties and skin penetration capabilities.
Alias	AN-2728, PF-06930164

Chemical Properties

Molecular Weight	251.05
Formula	C14H10BNO3
Cas No.	906673-24-3

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (199.16 mM)

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	3.9833 mL	19.9164 mL	39.8327 mL	199.1635 mL
5 mM	0.7967 mL	3.9833 mL	7.9665 mL	39.8327 mL
10 mM	0.3983 mL	1.9916 mL	3.9833 mL	19.9164 mL
20 mM	0.1992 mL	0.9958 mL	1.9916 mL	9.9582 mL
50 mM	0.0797 mL	0.3983 mL	0.7967 mL	3.9833 mL
100 mM	0.0398 mL	0.1992 mL	0.3983 mL	1.9916 mL

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In Vivo Formulation Calculator (Clear solution)

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DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

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Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

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Tech Support

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