Biological Activity
Potent and highly selective ROCK inhibitor (IC50 values are 0.6 and 1.1 nM for ROCK1 and ROCK2, respectively). Exhibits >200-fold selectivity over TRK and FLT3 receptors, and >900-fold selectivity over a panel of other kinases and cardiovascular relevent enzymes and receptors. Reduces blood pressure in normotensive and hypertensive rats. Orally active.
Technical Data
| M. Wt | 402.79 |
| Formula | C18H13ClF2N6O |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 867017-68-3 |
| PubChem ID | 11524200 |
| InChI Key | NRSGWEVTVGZDFC-UHFFFAOYSA-N |
| Smiles | ClC1=CC(NC2=CC(F)=C(OC3=C(C(C)=CN4)C4=NC=C3)C(F)=C2)=NC(N)=N1 |
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 | 40.28 | 100 | |
| ethanol | 40.28 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 402.79. 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 | 2.48 mL | 12.41 mL | 24.83 mL |
| 5 mM | 0.5 mL | 2.48 mL | 4.97 mL |
| 10 mM | 0.25 mL | 1.24 mL | 2.48 mL |
| 50 mM | 0.05 mL | 0.25 mL | 0.5 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Kast et al (2007) Cardiovascular effects of a novel potent and highly selective azaindole-based inhibitor of Rho-kinase. Br.J.Pharmacol. 152 1070 PMID: 17934515
Dahal et al (2010) Therapeutic efficacy of azaindole-1 in experimental pulmonary hypertension. Eur.Resp.J. 36 808 PMID: 20530035
Keywords: TC-S 7001, supplier, TC-S7001, Azaindole-1, potent, selective, rho-kinase, inhibitors, inhibits, ROCK1, ROCK2, Azaindole-1, Rho-kinases, Rho-kinases, Tocris Bioscience
