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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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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.
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.
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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- 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