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Submit ReviewNKH 477
Description: Water-soluble adenylyl cyclase activator
Alternative Names: Colforsin dapropate hydrochloride, 6-(3-dimethylaminopropionyl)forskolin hydrochloride
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% (HPLC)
Biological Activity for NKH 477
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 for NKH 477
| M. Wt | 546.1 |
| Formula | C27H43NO8.HCl |
| Storage | Desiccate at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 138605-00-2 |
| PubChem ID | 444028 |
| InChI Key | VIRRLEDAYYYTOD-YHEOSNBFSA-N |
| Smiles | O=C(CCN(C)C)O[C@H]2[C@@]1([H])C(C)(C)CC[C@H](O)[C@@](C)1[C@]3(O)[C@@](O[C@](C=C)(C)CC3=O)(C)[C@H]2OC(C)=O.Cl |
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.
Solubility Data for NKH 477
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 21.84 | 40 |
Preparing Stock Solutions for NKH 477
The following data is based on the product molecular weight 546.1. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.4 mM | 4.58 mL | 22.89 mL | 45.78 mL |
| 2 mM | 0.92 mL | 4.58 mL | 9.16 mL |
| 4 mM | 0.46 mL | 2.29 mL | 4.58 mL |
| 20 mM | 0.09 mL | 0.46 mL | 0.92 mL |
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Product Datasheets for NKH 477
References for NKH 477
References are publications that support the biological activity of the product.
Hosono et al (1992) Cardiovascular and adenylate cyclase stimulant properties of NKH477, a novel water-soluble forskolin derivative. J.Cardiovasc.Pharmacol. 19 625 PMID: 1380607
Satake et al (1998) Relaxant effects of NKH477, a new water-soluble forskolin derivative, on guinea-pig tracheal smooth muscle: the role of Ca2+-activated K+ channels. Br.J.Pharmacol. 123 753 PMID: 9517396
Toya et al (1998) Forskolin derivatives with increased selectivity for cardiac adenylyl cyclase. J.Mol.Cell.Cardiol. 30 97 PMID: 9500868
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Keywords: NKH 477, NKH 477 supplier, Water-soluble, adenylyl, adenylate, cyclases, activators, cAMP, NKH477, Colforsin, dapropate, hydrochloride, 6-(3-dimethylaminopropionyl)forskolin, Adenylyl, Cyclase, Enzyme, Substrates, /, Activators, 1603, Tocris Bioscience
7 Citations for NKH 477
Citations are publications that use Tocris products. Selected citations for NKH 477 include:
Xia et al (2011) Inhibition of morphine-induced cAMP overshoot: a cell-based assay model in a high-throughput format. PLoS One 31 901 PMID: 21598037
Lee et al (2012) The calcium-sensing receptor regulates the NLRP3 inflammasome through Ca2+ and cAMP. Nature 492 123 PMID: 23143333
Park et al (2016) Pyrin inflammasome activation and RhoA signaling in the autoinflammatory diseases FMF and HIDS. Nat Immunol 17 914 PMID: 27270401
Zhong et al (2012) Phosphodiesterase 4 inhibition impairs cocaine-induced inhibitory synaptic plasticity and conditioned place preference. Neuropsychopharmacology 37 2377 PMID: 22713909
Frieling (2017) Matrix metalloproteinase processing of PTHrP yields a selective regulator of osteogenesis, PTHrP1-17. Oncogene 36 4498 PMID: 28368420
Muschter et al (2015) Sympathetic Neurotransmitters Modulate Osteoclastogenesis and Osteoclast Activity in the Context of Collagen-Induced Arthritis. PLoS One 10 e0139726 PMID: 26431344
Brosnahan et al (2013) NE potentiates proinflammatory responses of human vaginal epithelial cells. Cell Mol Neurobiol 259 42583 PMID: 23571017
Do you know of a great paper that uses NKH 477 from Tocris? Please let us know.
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