L 858051 dihydrochloride  (Synonyms: 7DMB-Forskolin)

L 858051 (7DMB-Forskolin) dihydrochloride, an analog of Forskolin (HY-15371), is an adenylyl cyclase stimulator. L 858051 dihydrochloride directly activates adenylyl cyclase to increase intracellular, cellular, and ciliary cAMP levels. L 858051 dihydrochloride activates recombinant cyclic nucleotide-gated (E583M CNGA2) channels to induce a non-selective, Mg²⁺-sensitive current in adult rat ventricular myocytes. L 858051 dihydrochloride maximally stimulates L-type Ca²⁺ current in adult rat ventricular myocytes. L 858051 dihydrochloride increases total PDE3 and PDE4 activities in adult rat ventricular myocytes, with effects insensitive to PKA inhibition. L 858051 dihydrochloride 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) dihydrochloride 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) dihydrochloride 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) dihydrochloride 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) dihydrochloride 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.

609.62

C₂₉H₅₀Cl₂N₂O₇

115116-37-5

O=C(O[C@H]1[C@@H](O)[C@@]2([H])C(C)(C)CC[C@H](O)[C@]2(C)[C@]3(O)[C@]1(C)O[C@@](C)(C=C)CC3=O)CCCN4CCN(C)CC4.Cl.Cl

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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]