Biological Activity
Potent Kir6 (KATP) channel opener (EC50 for relaxation of rat aorta = 7.5 nM). Binds to SUR2A and SUR2B with high affinity (Kd values are 17 and 3 nM respectively).
Technical Data
| M. Wt | 231.3 |
| Formula | C12H17N5 |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 60559-98-0 |
| PubChem ID | 43345 |
| InChI Key | HKZNADVVGXKQDL-UHFFFAOYSA-N |
| Smiles | CCC(C)(C)N=C(/NC#N)NC1=CC=CN=C1 |
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 | 23.13 | 100 | |
| ethanol | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 231.3. 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 | 4.32 mL | 21.62 mL | 43.23 mL |
| 5 mM | 0.86 mL | 4.32 mL | 8.65 mL |
| 10 mM | 0.43 mL | 2.16 mL | 4.32 mL |
| 50 mM | 0.09 mL | 0.43 mL | 0.86 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Ashcroft and Gribble (2000) New windows on the mechanism of action of KATP channel openers. TiPS 21 439 PMID: 11121575
Buckner et al (2000) Pharmacological and molecular analysis of ATP-sensitive K+ channels in the pig and human detrusor. Eur.J.Pharmacol. 400 287 PMID: 10988346
Gross et al (1999) Stoichiometry of potassium channel opener action. Mol.Pharmacol. 56 1370 PMID: 10570067
Higdon et al (1997) Tissue and species variation in the vascular receptor binding of 3H-P1075, a potent KATP opener vasodilator. J.Pharmacol.Exp.Ther. 280 255 PMID: 8996204
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