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Postion:Product Catalog >Biochemical Engineering>Inhibitors> Crisaborole
	Crisaborole
  • 	Crisaborole
  • 	Crisaborole

Crisaborole NEW

Price $30 $0.8
Package 1kg 1000kg
Min. Order: 1kg
Supply Ability: g-kg-tons, free sample is available
Update Time: 2024-03-26

Product Details

Product Name: Crisaborole CAS No.: 906673-24-3
Min. Order: 1kg Purity: 99%
Supply Ability: g-kg-tons, free sample is available Release date: 2024/03/26
Lead time: In stock, ready for shipment Package: bag/bottle/drum/IBC
Delivery: By express, by air, by sea Origin: Manufacturer, advantage product
COA, MSDS: Available, contact us for details Name: Sun

1. Materials information

Names

Name4-((1-Hydroxy-1,3-dihydrobenzo[c][1,2]oxaborol-5-yl)oxy)benzonitrile
SynonymMore Synonyms

 AN-2728 Biological Activity

DescriptionCrisaborole (AN-2728) is a potent inhibitor of PDE4 and cytokine release; inhibit PDE4 with an IC50 of 0.49 μM.
Related Catalog
Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphodiesterase (PDE)
Research Areas >> Inflammation/Immunology
Target

IC50: 0.49 μM (PDE4)[1]

In VitroCrisaborole (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].
In VivoCrisaborole (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].
References

[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.

[3]. 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.

 Chemical & Physical Properties

Density1.3±0.1 g/cm3
Boiling Point425.9±55.0 °C at 760 mmHg
Molecular FormulaC14H10BNO3
Molecular Weight251.045
Flash Point211.4±31.5 °C
Exact Mass251.075378
PSA62.48000
LogP1.56828
Vapour Pressure0.0±1.1 mmHg at 25°C
Index of Refraction1.629
Storage condition-20°C

 Safety Information

HS Code2926909090

 Customs

HS Code2926909090
SummaryHS:2926909090 other nitrile-function compounds VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:30.0%

 Synonyms

AN2728
AN-2728
Crisaborole
UNII-Q2R47HGR7P
4-[(1-hydroxy-3H-2,1-benzoxaborol-5-yl)oxy]benzonitrile
Benzonitrile, 4-[(1,3-dihydro-1-hydroxy-2,1-benzoxaborol-5-yl)oxy]-
4-[(1-Hydroxy-1,3-dihydro-2,1-benzoxaborol-5-yl)oxy]benzonitrile
4-[(1,3-Dihydro-1-hydroxy-2,1-benzoxaborol-5-yl)oxy]benzonitrile

2. Packaging of materials

  • For powders: normal is 25kgs/Drum or bag, or larger/smaller package as request.

  • For liquids: normal 25kgs/drum, 180-300kgs/bucket, or IBC, determined by the nature of the product. 

                             Or smaller package 1kg/bottle, 10kgs/bottle as request. 


Article illustrationArticle illustration


3. Shipping & Delivery

  • By Express

Provide door to door service

Suitable for goods under 50kg

Delivery: 3-7 days

Cost: low cost

Article illustration


  • By Air

Provide airport to airport service

Suitable for goods over 50kg

Delivery: 3-14 days

Cost: high cost

Article illustration


  • By Sea

Provide seaport to seaport service

Suitable for goods over 100kg

Delivery: 2-45 days

Cost: low cost

Article illustration


4. Contact information

For more details, pls contact us freely.

Email address: sun@fdachem.com

Mob: 86 13526505137

WhatsApp/Skype/Wechat/LINE: 86 13526505137





Company Profile Introduction

Henan Fengda Chemical Co., Ltd. is located in the High-tech Development Zone of Henan Province. Specializing in the production and sales of various fine chemical products required for industrial production, including chemical raw materials, organic raw materials, petrochemicals, chemical reagents, solvents, catalysts, and additives, etc.

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  • Since: 2023-02-10
  • Address: Room 01, 2288 E05, Building 14, East Henan University, Science and Technology Park, 279 Xisanhuan Ro
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