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.
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- CAS No.: 110452-75-0
- Formule: C29H48N2O7
- Masse moléculaire:536.70
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS No. 110452-75-0
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Masse moléculaire 536.70
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Formule C29H48N2O7
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SMILES
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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Synonyms
7DMB-Forskolin free base
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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Ca2+ Staining Technique
Ca2+ staining is an experimental technique that utilizes specific fluorescent probes (such as Fluo-4 AM, Fura-2, etc.) to qualitatively or quantitatively detect dynamic changes in intracellular Ca2+ concentrations; this is achieved by monitoring the changes in fluorescent signals generated when these probes bind to free intracellular calcium ions. The underlying principle relies primarily on the presence of chelating groups within the probe's molecular structure that possess high affinity for calcium ions.
Pureté et documentation
Références
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
L 858051 Related Classifications
HY-116540 Related Classifications
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Keywords
- L 858051
- 110452-75-0
- 7DMB-Forskolin
- L858051
- L-858051
- Adenylate Cyclase
- phosphodiesterase inhibitor IBMX
- cAMP
- PDE3
- L-type Ca2+ current
- rat lacrimal gland acinar cells
- mouse embryonic fibroblasts
- p44/p42 mitogen-activated protein kinase
- adenylyl cyclase
- adult rat ventricular myocytes
- cyclic nucleotide-gated (E583M CNGA2) channels
- Inhibitor
- inhibitor
- inhibit