| Bioactivity | Difamilast (OPA-15406) is a topical, selective and nonsteroidal phosphodiesterase-4 (PDE4) inhibitor with particularly efficient inhibition of subtype B (IC50=11.2 nM). Difamilast can be used for the research of mild to moderate atopic dermatitis (AD)[1][2][3]. | ||||||||||||
| Invitro | OPA-15406 is highly selective for inhibition of PDE4 subtype B (IC50=11.2 nM), and OPA-15406 also exerts inhibitory effects on PDE2[2]. | ||||||||||||
| In Vivo | OPA-1540 improves skin condition in relevant animal models of AD[1]. | ||||||||||||
| Name | Difamilast | ||||||||||||
| CAS | 937782-05-3 | ||||||||||||
| Formula | C23H24F2N2O5 | ||||||||||||
| Molar Mass | 446.44 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Hanifin JM, et, al. OPA-15406, a novel, topical, nonsteroidal, selective phosphodiesterase-4 (PDE4) inhibitor, in the treatment of adult and adolescent patients with mild to moderate atopic dermatitis (AD): A phase-II randomized, double-blind, placebo-con [2]. Ahluwalia J, et, al. Phosphodiesterase 4 Inhibitor Therapies for Atopic Dermatitis: Progress and Outlook. Drugs. 2017 Sep;77(13):1389-1397. [3]. Soeberdt M, et, al. Small molecule drugs for the treatment of pruritus in patients with atopic dermatitis. Eur J Pharmacol. 2020 Aug 15;881:173242. |