L 858051 dihydrochloride
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.
For research use only. We do not sell to patients.
- CAS No.: 115116-37-5
- Formula: C29H50Cl2N2O7
- Molecular Weight:609.62
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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.
Chemical Information
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CAS No. 115116-37-5
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Molecular Weight 609.62
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Formula C29H50Cl2N2O7
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SMILES
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
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Synonyms
7DMB-Forskolin
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[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 dihydrochloride Related Classifications
HY-116540A Related Classifications
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- L 858051
- 115116-37-5
- 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