L 858051  (Synonyms: 7DMB-Forskolin free base)

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].

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

536.70

C₂₉H₄₈N₂O₇

110452-75-0

O=C(CCCN1CCN(CC1)C)O[C@H]2[C@H]([C@]3(C(C)(CC[C@@H]([C@@]3([C@@]4([C@@]2(O[C@@](C=C)(CC4=O)C)C)O)C)O)C)[H])O

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• [1]. Funaki C, et al. Role of cAMP inhibition of p44/p42 mitogen-activated protein kinase in potentiation of protein secretion in rat lacrimal gland. Am J Physiol Cell Physiol. 2007;293(5):C1551-C1560.  [Content Brief]

  [2]. Moore BS, et al. Cilia have high cAMP levels that are inhibited by Sonic Hedgehog-regulated calcium dynamics. Proc Natl Acad Sci U S A. 2016;113(46):13069-13074.  [Content Brief]

  [3]. Rochais F, et al. Negative feedback exerted by cAMP-dependent protein kinase and cAMP phosphodiesterase on subsarcolemmal cAMP signals in intact cardiac myocytes: an in vivo study using adenovirus-mediated expression of CNG channels. J Biol Chem. 2004 Dec 10;279(50):52095-105.  [Content Brief]