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Submit ReviewPNU 37883 hydrochloride is a novel antagonist selective for the vascular form of Kir6 (KATP) channel; inhibits Kir6 currents in isolated mesenteric artery smooth muscle cells (Kd = 65 nM) but not in cardiac or skeletal myocytes. Inhibits blood vessel relaxation and hypotension induced by pinacidil in vivo. Displays weak diuretic effects.
PNU 37883 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
M. Wt | 381.98 |
Formula | C21H35N3O.HCl |
Storage | Desiccate at RT |
Purity | ≥99% (HPLC) |
CAS Number | 57568-80-6 |
PubChem ID | 64392 |
InChI Key | FZALCKUJYZCDOX-UHFFFAOYSA-N |
Smiles | C1(CC3C2)CC2(/N=C(N5CCOCC5)/NC4CCCCC4)CC(C3)C1.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.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 9.55 | 25 | |
ethanol | 38.2 | 100 |
The following data is based on the product molecular weight 381.98. 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 |
---|---|---|---|
1 mM | 2.62 mL | 13.09 mL | 26.18 mL |
5 mM | 0.52 mL | 2.62 mL | 5.24 mL |
10 mM | 0.26 mL | 1.31 mL | 2.62 mL |
50 mM | 0.05 mL | 0.26 mL | 0.52 mL |
References are publications that support the biological activity of the product.
Humphrey and Ludens (1998) KATP-blocking diuretic PNU-37883A reduces plasma renin activity in dogs. J.Cardiovasc.Pharmacol. 31 894 PMID: 9641474
Cui et al (2003) Different molecular sites of action for the KATP channel inhibitors, PNU-99963 and PNU-37883A. Br.J.Pharmacol. 139 122 PMID: 12746230
Kovalev et al (2004) Molecular analysis of the subtype-selective inhibition of cloned KATP channels by PNU-37883A. Br.J.Pharmacol. 141 867 PMID: 14757705
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Keywords: PNU 37883 hydrochloride, PNU 37883 hydrochloride supplier, Vascular, KATP, channels, blockers, Potassium, KIR, Inward, Rectifier, K+, PNU37883, hydrochloride, antagonist, Kir6, rectifier, Channels, 2095, Tocris Bioscience
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Average Rating: 4 (Based on 1 Review.)
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PNU 37883 was used to understand whether it shows BK channel blocking effect. The product worked ideally although inhibition data obtained from the product shows variation.
I suggest using an alternate channel blocker to measure blocking action to identify the variation with PNU 37883.