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Crisaborole

Catalog No. T4285 CAS 906673-24-3

Synonyms: AN-2728, PF-06930164

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

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Crisaborole, CAS 906673-24-3

Pack Size	Availability	Price/USD
10 mg	In stock	$ 38.00
50 mg	In stock	$ 50.00
100 mg	In stock	$ 83.00
200 mg	In stock	$ 111.00
1 mL * 10 mM (in DMSO)	In stock	$ 46.00

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Purity: 99.91%

Biological Description

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Storage & Solubility Information

Description	Crisaborole (AN-2728) is a Phosphodiesterase 4 Inhibitor.
Targets&IC50	PDE4:0.49 μM
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.

Synonyms	AN-2728, PF-06930164
Molecular Weight	251.05
Formula	C14H10BNO3
CAS No.	906673-24-3

Storage

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

Solubility Information

DMSO: 32 mg/mL

References and Literature

1. Akama T, et al. Discovery and structure-activity study of a novel benzoxaborole anti-inflammatory agent (AN2728) for the potential topical treatment of psoriasis and atopic dermatitis. Bioorg Med Chem Lett. 2009 Apr 15;19(8):2129-32. 2. Nazarian R, et al. AN-2728, a PDE4 inhibitor for the potential topical treatment of psoriasis and atopic dermatitis. Curr Opin Investig Drugs. 2009 Nov;10(11):1236-42.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Drug Repurposing Compound Library EMA Approved Drug Library Anti-Neurodegenerative Disease Compound Library FDA-Approved & Pharmacopeia Drug Library Anti-Cardiovascular Disease Compound Library Drug-Fragment Library Bioactive Lipid Compound Library Clinical Compound Library Bioactive Compound Library

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Keywords

Crisaborole 906673-24-3 Metabolism PDE Inhibitor inhibit AN 2728 PF06930164 AN2728 AN-2728 PF 06930164 Phosphodiesterase (PDE) PF-06930164 inhibitor

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