Biological Activity
Kir6 (KATP) channel opener and active metabolite of Y-27152 (Cat. No. 2077). Relaxes contracted rat aortic rings (IC50 = 0.027 mM) and inhibits glucose-induced insulin secretion in isolated human pancreatic β-cells in vitro. Produces hypotension in spontaneously hypertensive rats and displays cardioprotective properties in dogs following systemic administration in vivo.
Technical Data
M. Wt | 276.29 |
Formula | C14H16N2O4 |
Storage | Store at RT |
Purity | ≥98% (HPLC) |
CAS Number | 127408-31-5 |
PubChem ID | 121878 |
InChI Key | IWTCFIIOUXJOOV-OLZOCXBDSA-N |
Smiles | CC(=O)N(O)[C@H]1[C@H](O)C(C)(C)OC2=C1C=C(C=C2)C#N |
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 | |||
1eq. NaOH | 27.63 | 100 | |
DMSO | 27.63 | 100 | |
ethanol | 27.63 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 276.29. 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 | 3.62 mL | 18.1 mL | 36.19 mL |
5 mM | 0.72 mL | 3.62 mL | 7.24 mL |
10 mM | 0.36 mL | 1.81 mL | 3.62 mL |
50 mM | 0.07 mL | 0.36 mL | 0.72 mL |
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References
References are publications that support the products' biological activity.
Nakajima et al (1992) Y-27152, a long-acting K+ channel opener with less tachycardia: antihypertensive effects in hypertensive rats and dogs in conscious state. J.Pharmacol.Exp.Ther. 261 730 PMID: 1578381
Fukunari et al (1997) Y-26763 protects the canine heart from a stunning injury through opening of the KATP channels Eur.J.Pharmacol. 323 197 PMID: 9128839
Cosgrove et al (2004) Y-26763: ATP-sensitive K+ channel activation and the inhibition of insulin release from human pancreatic β-cells Eur.J.Pharmacol. 486 133 PMID: 14975702
Keywords: Y-26763, supplier, KATP, channel, openers, Potassium, KIR, Inward, Rectifier, K+, Kir6, Inward, rectifier, Potassium, Channels, Inward, rectifier, Potassium, Channels, Tocris Bioscience