Biological Activity
α2-adrenoreceptor antagonist (Kd values are; 0.18, 0.19 and 0.42 nM for α2B α2C and α2A, respectively in rat).
Licensing Information
Sold with the permission of Roche Bioscience
Technical Data
| M. Wt | 400.96 |
| Formula | C19H28N2O3S.HCl |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 186002-54-0 |
| PubChem ID | 9908991 |
| InChI Key | DZTZUOBWDBPPJQ-BQBHMPFISA-N |
| Smiles | [H][C@]12C4=C(C=C(OC)C=C4)CCN1C[C@]3([H])[C@](N(S(=O)(CC)=O)CCC3)([H])C2.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
| Solubility | Soluble to 25 mM in water |
Preparing Stock Solutions
The following data is based on the product molecular weight 400.96. 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 | 2.49 mL | 12.47 mL | 24.94 mL |
| 5 mM | 0.5 mL | 2.49 mL | 4.99 mL |
| 10 mM | 0.25 mL | 1.25 mL | 2.49 mL |
| 50 mM | 0.05 mL | 0.25 mL | 0.5 mL |
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References
References are publications that support the products' biological activity.
Clark et al (1989) (8aα,12aα,13aα)-5,8,8a,9,10,11,12,12a,13,13a-Decahydro-3-methoxy-12-(ethylsulphonyl)-6H-isoquino[2,1-g][1,6]-naphthyridine, a potent and highly selective α2-adrenoceptor antagonist. J. Med. Chem. 32 2034 PMID: 2570150
Hume et al (1996) Evaluation in rat of RS-79948-197 as a potential PET ligand for central α2-adrenoceptors. Eur.J.Pharmacol. 317 67 PMID: 8982721
Uhlen et al (1998) [3H]RS79948-197 binding to rat, guinea pig and pig α2A-, α2B and α2C-adrenoceptors. Comparison with MK912, RX821002, rauwolscine and yohimbine. Eur.J.Pharmacol. 343 93 PMID: 9551719
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