pde4b-in-2

PDE4B-IN-2 (A 33) is an orally active and selective PDE4B inhibitor with an IC50 of 15 nM. PDE4B-IN-2 inhibits PDE4D (IC50=1.7 µM). PDE4B-IN-2 exhibits potent anti-inflammatory effects.

This compound is a dual 5-HT1A 5-HT7 receptor antagonist (5-HT1A Ki = 8 nM, Kb = 0.04 nM; 5-HT7 Ki = 451 nM, Kb = 460 nM) with additional inhibitory activity against PDE4B PDE7A (PDE4B IC50 = 80.4 μM; PDE7A IC50 = 151.3 μM). Its antidepressant-like effect surpasses that of the reference agent, escitalopram.

PDE4B D-IN-2 (example 19) serves as a highly effective inhibitor of PDE4, exhibiting IC50 values of 0.023 nM for PDE4B2 and 0.066 nM for PDE4D.

LEO 39652, a dual-soft PDE4 inhibitor, demonstrates potent inhibition of PDE4 subtypes A, B, C, and D with respective IC50 values of 1.2 nM, 1.2 nM, 3.0 nM, and 3.8 nM. Additionally, it inhibits TNF-α with an IC50 of 6.0 nM, indicating its potential for topical Atopic dermatitis (AD) research [1].