Biological Activity
α2C-adrenoceptor antagonist that displays ~ 50-fold selectivity over other α2-adrenoceptor subtypes (Ki values are 28, 1470, 1700 and 3150 nM for human α2C, α2B, α2D and α2A subtypes respectively). Potently antagonizes adrenalin-stimulated 35GTPγS binding in vitro (KB = 16 nM) and produces antidepressant and antipsychotic-like effects in vivo.
Technical Data
M. Wt | 441.4 |
Formula | C24H24N4.2HCl |
Storage | Desiccate at -20°C |
Purity | ≥99% (HPLC) |
CAS Number | 1259314-65-2 |
PubChem ID | 49855035 |
InChI Key | VVZOADYFJAJZGL-UHFFFAOYSA-N |
Smiles | CN(CC5)CCN5C(C=C4)=CC=C4NC2=C3C(C=CC=C3)=NC1=CC=CC=C12.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 | |||
DMSO | 2.2 | 5 | |
water | 44.14 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 441.4. 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 | 11.33 mL | 22.66 mL |
5 mM | 0.45 mL | 2.27 mL | 4.53 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.
Tricklebank (2007) JP-1302: a new tool to shed light on the roles of α2C-adrenoceptors in brain. Br.J.Pharmacol. 150 381 PMID: 17220912
Sallinen et al (2007) Pharmacological characterization and CNS effects of a novel highly selective α2C-adrenoceptor antagonist JP-1302. Br.J.Pharmacol. 150 391 PMID: 17220913
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