Adapalene

A cell-permeable naphthoic acid compound that exhibits selective affinity and agonistic potency toward RARβ and RARγ over RARα (Kd = 34, 130, and 1100 nM, respectively; AC₅₀ = 2.3, 9.3, and 22 nM, respectively, in COS-7-based reporter assays) without appreciable affinity toward cytosolic retinoic acid binding proteins CRABP I/II (Kd >>1 M) or detectable activity toward RXRα (AC₅₀ >1 M). The biological activity and pharmaceutical efficacy of ADA are generally shown to be superior to those of ATRA/Tretinoin both in vitro and in vivo.

A cell-permeable naphthoic acid compound that exhibits selective affinity and agonistic potency toward RARβ and RARγ over RARα (Kd = 34, 130, and 1100 nM, respectively; AC₅₀ = 2.3, 9.3, and 22 nM, respectively, in COS-7-based reporter assays) without appreciable affinity toward cytosolic retinoic acid binding proteins CRABP I/II (Kd >>1 µM) or detectable activity toward RXRα (AC₅₀ >1 µM). The biological activity and pharmaceutical efficacy of ADA are generally shown to be superior to those of ATRA/Tretinoin (Cat. No. 554720) both in vitro and in vivo.

Toxicity: Standard Handling (A)

Following initial thaw, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

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Shroot, B., et al. 1997. J. Am. Acad. Dermatol.36, S96.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany