Biological Activity
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.
Compound Libraries
PNU 37883 hydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| 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.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 9.55 | 25 | |
| ethanol | 38.2 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 381.98. 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.
| 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 |
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Product Datasheets
References
References are publications that support the products' biological activity.
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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