Biological Activity
Potent and selective α2D-adrenoceptor agonist (Ki values are 8.6 pM and 110 nM for rat α2D and α1 receptors respectively and 25, 26 and 100 nM for human α2A, α2C and α2B receptors respectively. Exhibits analgesic activity in a mouse model of abdominal irritation. Orally active.
Compound Libraries
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Technical Data
| M. Wt | 346.4 |
| Formula | C13H14N2S.C4H4O4 |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 245744-18-7 |
| PubChem ID | 90488997 |
| InChI Key | OPCJPAYHMCWCGW-BTJKTKAUSA-N |
| Smiles | CC1=C2C(C(C3=CNC=N3)=CCC2)=C(C)S1.O=C(C=C/C(O)=O)O |
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 | 34.64 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 346.4. 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 | 2.89 mL | 14.43 mL | 28.87 mL |
| 5 mM | 0.58 mL | 2.89 mL | 5.77 mL |
| 10 mM | 0.29 mL | 1.44 mL | 2.89 mL |
| 50 mM | 0.06 mL | 0.29 mL | 0.58 mL |
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References
References are publications that support the products' biological activity.
Ross et al (2000) α2 adrenoceptor agonists as potential analgesic agents. 2. Discovery of 4-(4-Imidazo)-1,3-dimethyl-6,7-dihydrothianaphthene as a high-affinity ligand for the α2D adrenergic receptor. J.Med.Chem. 43 1423 PMID: 10715142
Keywords: TC-G 1000, supplier, TC-G1000, potent, selective, adrenergic, receptors, agonists, alpha2d, alpha1, alpha2a, alpha2b, alpha2c, α2d, α2a, α1, α2b, α2c, adrenoceptors, Adrenergic, Alpha-2, Receptors, Adrenergic, Alpha-2, Receptors, Tocris Bioscience
