Biological Activity
Potent TRPC6 inhibitor (IC50 values are 9.5, 226 and 282 nM for TRPC6, TRPC7 and TRPC3-mediated Ca2+ influx). Exhibits no significant activity at TRPC4 and TRPC5 channels. Suppresses TRPC6-dependent acute hypoxic pulmonary vasoconstriction (HPV) in the isolated perfused mouse lung. Orally bioavailable.
Technical Data
| M. Wt | 440.79 |
| Formula | C21H22ClN3O.2HCl |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1333207-63-8 |
| Smiles | N[C@@H]1CCCN([C@@H]2CC3=CC=CC=C3[C@H]2OC4=C(C=C(C#N)C=C4)Cl)C1.Cl.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 | |||
| water | 44.08 | 100 | |
| DMSO | 44.08 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 440.79. 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 | 2.27 mL | 11.34 mL | 22.69 mL |
| 5 mM | 0.45 mL | 2.27 mL | 4.54 mL |
| 10 mM | 0.23 mL | 1.13 mL | 2.27 mL |
| 50 mM | 0.05 mL | 0.23 mL | 0.45 mL |
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References
References are publications that support the products' biological activity.
Maier et al (2015) Discovery and pharmacological characterization of a novel potent inhibitor of diacylglycerol-sensitive TRPC cation channels. Br.J.Pharmacol. 172 3650 PMID: 25847402
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