Tanimilast

Tanimilast (CHF-6001) is an orally active and selective phosphodiesterase 4 inhibitor (IC₅₀=0.026 nM) with robust anti-inflammatory activity and suitable for topical pulmonary administration. Tanimilast increases cellular cAMP levels, and inhibits NF-κB signaling pathway. Tanimilast is used for the research of obstructive lung diseases^[1][2]. In Vitro: Tanimilast (0.1 nM-0.1 μM, 24 h) increases the expression of CCR7 protein; inhibits the production of cytokines such as TNF-α, IL-1β, IL-6, IL-12, and IL-23; reduces the production of chemokines such as CXCL8, CCL3, CXCL10, and CCL19, IC₅₀s in LPS (HY-D1056)-stimulated human monocyte-derived dendritic cells are 0.5, 4.6, 2.8, 1.7, 9.3, 7.2, 1.2, 1.8 and 0.8 nM, respectively^[2].
In Vivo: Tanimilast (100-600 µg/kg, dry powder inhalation, single dose) ameliorates LPS (HY-D1056)-induced acute pulmonary inflammation in mouse models^[3].