Crisaborole Impurity 16 Chemical Properties

form 

Solid

color 

Off-white to light yellow

Crisaborole Impurity 16 Usage And Synthesis

Uses

Crisaborole-d4 is deuterium labeled Crisaborole. Crisaborole (AN-2728) is a potent inhibitor of PDE4 and cytokine release; inhibit PDE4 with an IC50 of 0.49 μM.

References

[1] 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. PMID:19876791
[2] Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. DOI:10.1177/1060028018797110
[3] 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. DOI:10.1016/j.bmcl.2009.03.007