110452-75-0
Chemical Structure
L 858051
Synonym(s): 7DMB-Forskolin free base
- CAS No.: 110452-75-0
- Formula:C29H48N2O7
- Molecular Weight:536.70
IUPAC Name: (3R,4aR,5S,6S,6aS,10S,10aR,10bS)-6,10,10b-trihydroxy-3,4a,7,7,10a-pentamethyl-1-oxo-3-vinyldodecahydro-1H-benzo[f]chromen-5-yl 4-(4-methylpiperazin-1-yl)butanoate
InChIKey: PAYHDZDDAHVPDU-ZQVYKFDISA-N
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
Biological Activity: 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[1][2][3].
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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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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]
