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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 110452-75-0
- 分子式: C29H48N2O7
- 分子量:536.70
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保管条件:
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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生物活性
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化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
体外実験
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.
化学情報
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CAS 番号 110452-75-0
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分子量 536.70
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分子式 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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別名
7DMB-Forskolin free base
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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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.
純度とドキュメンテーション
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
L 858051 関連分類
HY-116540 関連分類
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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