NKH 477

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Cat.No. 1603 - NKH 477 | C27H43NO8.HCl | CAS No. 138605-00-2
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)
Datasheet
Citations (5)
Literature

Biological Activity

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. Also available as part of the PKA Tocriset™.

Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 54.61 100
ethanol 8.19 15
water 21.84 40

Preparing Stock Solutions

The following data is based on the product molecular weight 546.1. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.83 mL 9.16 mL 18.31 mL
5 mM 0.37 mL 1.83 mL 3.66 mL
10 mM 0.18 mL 0.92 mL 1.83 mL
50 mM 0.04 mL 0.18 mL 0.37 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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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View Related Products by Product Action

View all Adenylyl Cyclase Activators

Keywords: Water-soluble adenylyl adenylate cyclases activators cAMP NKH477 Colforsin dapropate hydrochloride 6-(3-dimethylaminopropionyl)forskolin hydrochloride Adenylyl Cyclase

5 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

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) Norepinephrine potentiates proinflammatory responses of human vaginal epithelial cells. Cell Mol Neurobiol 259 42583 PMID: 23571017

Lee et al (2012) The calcium-sensing receptor regulates the NLRP3 inflammasome through Ca2+ and cAMP. Nature 492 123 PMID: 23143333


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Literature in this Area

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