Biological Activity
Potent and selective vasopressin V1B antagonist (Ki values are 3.7 and 1.3 nM for native and recombinant rat V1b receptors, respectively). Displays >70-fold selectively for rat V1B over V1A, V2 oxytoxin and a range of other receptors and ion channels. Inhibits AVP-induced glucagon release in In-R1-G9 α-pancreatic cells in vitro. Inhibits stress-induced ACTH release and exhibits anxiolytic-like effects in anxiety models. Orally bioavailable.
Technical Data
| M. Wt | 630.11 |
| Formula | C30H32ClN3O8S |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 439687-69-1 |
| PubChem ID | 9895468 |
| InChI Key | NJXZWIIMWNEOGJ-WEWKHQNJSA-N |
| Smiles | COC1=CC(OC)=C(S(=O)(N2C([C@@](C3=CC(Cl)=CC=C23)(C4=C(C=CC=C4)OC)N5C[C@@H](C[C@H]5C(N(C)C)=O)O)=O)=O)C=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 | 63.01 | 100 | |
| ethanol | 63.01 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 630.11. 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 | 1.59 mL | 7.94 mL | 15.87 mL |
| 5 mM | 0.32 mL | 1.59 mL | 3.17 mL |
| 10 mM | 0.16 mL | 0.79 mL | 1.59 mL |
| 50 mM | 0.03 mL | 0.16 mL | 0.32 mL |
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References
References are publications that support the products' biological activity.
Serradeil-Le Gal et al (2005) An overview of SSR149415, a selective nonpeptide vasopressin V1b receptor antagonist for the treatment of stress-related disorders. CNS Drug Rev. 11 53 PMID: 15867952
Keywords: SSR 149415, supplier, SSR149415, vasopressin, receptor, V1b, potent, selective, antagonists, antagonism, orally, bioavailable, Nelivaptan, Vasopressin, Receptors, Vasopressin, Receptors, Tocris Bioscience
