NKH 477
Chemical Name: N,N-Dimethyl-(3R,4aR,5S,6aS,10S,10aR,10bS)-5-(acetyloxy)-3-ethenyldodecahydro-10,10b-dihydroxy-3,4a,7,7,10a-pentamethyl-1-oxo-1H-naphtho[2,1-b]pyran-6-yl ester β-alanine hydrochloride
Purity: ≥98%
Biological Activity
NKH 477 is a water-soluble analog of forskolin (Cat. No. 1099) that is a potent activator of adenylyl cyclase; shows some selectivity for cardiac (type V) adenylyl cyclase. Stimulates bronchodilation (EC50 = 32.6 nM) and is an orally active potent positive chronotrope and hypotensive agent in vivo.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Matrix metalloproteinase processing of PTHrP yields a selective regulator of osteogenesis, PTHrP1-17
JS Frieling, G Shay, V Izumi, ST Aherne, RG Saul, M Budzevich, J Koomen, CC Lynch
Oncogene, 2017;0(0):. -
The calcium-sensing receptor regulates the NLRP3 inflammasome through Ca2+ and cAMP.
Lee G, Subramanian N, Kim A, Aksentijevich I, Goldbach-Mansky R, Sacks D, Germain R, Kastner D, Chae J
Nature, 2012;492(7427):123-7. -
Cardiovascular and adenylate cyclase stimulant properties of NKH477, a novel water-soluble forskolin derivative.
Hosono et al.
J.Cardiovasc.Pharmacol., 1992;19:625 -
Relaxant effects of NKH477, a new water-soluble forskolin derivative, on guinea-pig tracheal smooth muscle: the role of Ca2+-activated K+ channels.
Satake et al.
Br.J.Pharmacol., 1998;123:753 -
Forskolin derivatives with increased selectivity for cardiac adenylyl cyclase.
Toya et al.
J.Mol.Cell.Cardiol., 1998;30:97
Product Datasheets
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Citations for NKH 477
The citations listed below are publications that use Tocris products. Selected citations for NKH 477 include:
7 Citations: Showing 1 - 7
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Matrix metalloproteinase processing of PTHrP yields a selective regulator of osteogenesis, PTHrP1-17.
Authors: Frieling
Oncogene 2017;36(31):4498
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Pyrin inflammasome activation and RhoA signaling in the autoinflammatory diseases FMF and HIDS.
Authors: Park Et al.
Nat Immunol 2016;17:914
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Sympathetic Neurotransmitters Modulate Osteoclastogenesis and Osteoclast Activity in the Context of Collagen-Induced Arthritis.
Authors: Muschter Et al.
PLoS One 2015;10:e0139726
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NE potentiates proinflammatory responses of human vaginal epithelial cells.
Authors: Brosnahan Et al.
Cell Mol Neurobiol 2013;259:42583
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The calcium-sensing receptor regulates the NLRP3 inflammasome through Ca2+ and cAMP.
Authors: Lee Et al.
Nature 2012;492:123
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Phosphodiesterase 4 inhibition impairs cocaine-induced inhibitory synaptic plasticity and conditioned place preference.
Authors: Zhong Et al.
Neuropsychopharmacology 2012;37:2377
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Inhibition of morphine-induced cAMP overshoot: a cell-based assay model in a high-throughput format.
Authors: Xia Et al.
PLoS One 2011;31:901
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