Crisaborole-AN-2728-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemECrisaboroleCat. No.: HY-10978CAS No.: 906673-24-3Synonyms: AN-2728; PF-06930164分式: CHBNO分量: 251.05作靶点: Phosphodiesterase (PDE)作通路: Metabolic Enzyme/Protease储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解

2、性数据体外实验 DMSO : 32 mg/mL (127.46 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 3.9833 mL 19.9164 mL 39.8327 mL5 mM 0.7967 mL 3.9833 mL 7.9665 mL10 mM 0.3983 mL 1.9916 mL 3.9833 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Crisabo

3、role (AN-2728)是有效地PDE4和cytokine释放抑制剂，抑制PDE4的 IC50 值为0.49 M。IC50 & Target IC50: 0.49 M (PDE4) 1体外研究Crisaborole (AN-2728) inhibits PDE4, TNF-, IL-2, IFN-, IL-5 and IL-10 with IC50 values of 0.49, 0.54, 0.61,1/2 Master of Small Molecules 您边的抑制剂师www.MedChemE0.83, 2.4 and 5.3 M. Crisaborole (AN-2728) sho

4、ws the most potent activity against PDE4 catalytic domain,but it also shows inhibition against PDE1A3, PDE3Cat, and PDE7A1. Crisaborole (AN-2728) inhibits PDEisozymes PDE1A3, PDE3Cat , PDE4Cat and PDE7A1 with IC50 values of 6.1, 6.4, 0.11 and 0.73 M 1.Crystallography reveals that interaction of benz

5、oxaboroles with the hydrophobic pocket in the PDE4 catalyticdomain increase their affinity for PDE4. These benzoxaboroles strongly suppresses the secretion ofcytokines associated with Ps and AD 2. Crisaborole (AN-2728) is a topically administered, boron-containing,anti-inflammatory compound that inh

6、ibits PDE4 activity and thereby suppresses the release of TNFalpha, IL-12, IL-23 and other cytokines 3.体内研究 Crisaborole (AN-2728) shows significant inhibition against the ear edema caused by phorbol ester afterdosing at 1 mg/ear2 (78% and 68%, respectively). The efficacy is comparable to that of dex

7、amethasone,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 ofefficacy, with results that are comparable to positive controls in clinical tr

8、ials 3.REFERENCES1. Akama T, et al. Discovery and structure-activity study of a novel benzoxaborole anti-inflammatory agent (AN2728) for the potentialtopical 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

9、for the potential topical treatment of psoriasis and atopic dermatitis. Curr Opin InvestigDrugs. 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 InvestigDrugs. 2009 Nov;10(11):1236-42.McePdfHeightCaution: Product has not been fully validated for medic