L 858051

L 858051 (7DMB-Forskolin free base), an analog of Forskolin (HY-15371), is an adenylyl cyclase stimulator. L 858051 directly activates adenylyl cyclase to increase intracellular, cellular, and ciliary cAMP levels. L 858051 activates recombinant cyclic nucleotide-gated (E583M CNGA2) channels to induce a non-selective, Mg²⁺-sensitive current in adult rat ventricular myocytes. L 858051 maximally stimulates L-type Ca²⁺ current in adult rat ventricular myocytes. L 858051 increases total PDE3 and PDE4 activities in adult rat ventricular myocytes, with effects insensitive to PKA inhibition. L 858051 serves as a tool to elevate intracellular cAMP for studying subsarcolemmal cAMP dynamics and compartmentation in adult rat ventricular myocytes^[1][2][3]. In Vitro:L 858051 (100 μM; 30 min) inhibits basal p44/p42 MAPK activity by 39% in freshly isolated rat lacrimal gland acinar cells^[1].
L 858051 (1-100 μM; 5 min-24 h) dose-dependently increases intracellular and ciliary cAMP levels in mouse embryonic fibroblasts when applied directly to activate adenylyl cyclase^[2].
L 858051 (0.1-300 μM; 24 h post infection) potently activates subsarcolemmal cAMP-sensitive CNG channels in Ad-CNG-infected adult rat ventricular myocytes with an EC₅₀ of 36.7 μM for E583M CNGA2^[3].
L 858051 (10 μM; 5 min) enhances PDE3 and PDE4 activities in Ad-CNG-infected adult rat ventricular myocytes via a PKA-independent mechanism^[3].