For research use only. Not for therapeutic Use.
<p>It is an epithelial channel blocker, it also blocks voltage-gated Na+ channels. It has an anti-hypertensive action.</p><br />Pyrazinoylguanidine<!–C<SUB>6</SUB>H<SUB>8</SUB>ClN<SUB>7</SUB>O .HCl–>, synthetic</br><p>It is a potassium-sparing diuretic, ion transporters, enzymes and receptors inhibitor. 10-<sup>6</sup> M reversibly inhibit Na<sup>+</sup> transport in Na<sup>+ </sup>channels of the high resistance apical plasma epithelial membrane, when added to the solution bathing this membrane. It has no effect on Na<sup>+</sup> transport in basolateral plasma membrane [3-4]. The Na+ channel is the only ion transporter inhibited by Amiloride with an IC<sub>50</sub> of less than 1 μM. IC<sub>50</sub> in urinary epithelia = 0.34 μM, evaluated by the method of Cuthbert et al. 1978 [1].<br /> it is a weak reversible inhibitor of Na<sup>+</sup>/Ca<sup>2+</sup> exchanger.<br /> IC<sub>50</sub> = 2 mM for Na<sup>+</sup>-coupled solute transport in brush border membrane vesicles from rabbit kidney cortex and in LLC-PK1/CL4 cells [5].</p></br>
| Catalog Number | A000184 |
| CAS Number | 2016-88-8 |
| Synonyms | NA |
| Molecular Formula | C6H8ClN7O • HCl |
| Purity | ≥95% |
| Target | Sodium channel |
| Storage | 3 years -20C powder |
| InChIKey | ACHKKGDWZVCSNH-UHFFFAOYSA-N |
| Reference | – Kleyman T.R. et al., /Amiloride and its analogs as tools in the study of ion transport./ J. Membr. Biol. (1988). 105:1-21<br /><br />- Garritsen A. et al., /Interaction of Amiloride and its analogs with Adenosine A1 receptors in calf bain/, Biochem Pharmacol. (1990). 40(4):827<br /><br />- Bently P.J., J. Physiol. (London) (1968). 195:317-330<br /><br />- Sariban-Sohraby S. et al., Am. J. Physiol. (1986). 250:C175-C190<br /><br />- Harris R.C. et al., Kidney Int. (1985). 27:310<br /><br /><br /><br /> |
