Biological Activity
Allosteric potentiator at the adenosine A1 receptor; acts via agonist-dependent and -independent mechanisms. Enhances agonist affinity for, and increased t½ of dissociation from, the receptor. Also inhibits basal and forskolin-stimulated adenylyl cyclase (AC) activity in A1 receptors expressed in CHO cells, possibly via direct potentiation of constitutive receptor activity or by direct inhibition of AC. Active in vivo.
Technical Data
| M. Wt | 299.31 |
| Formula | C14H12F3NOS |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 132861-87-1 |
| PubChem ID | 122028 |
| InChI Key | KKDKAWKYGCUOGR-UHFFFAOYSA-N |
| Smiles | CC1=C(C)C(C(=O)C2=CC(=CC=C2)C(F)(F)F)=C(N)S1 |
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 | 29.93 | 100 | |
| ethanol | 29.93 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 299.31. 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 | 3.34 mL | 16.71 mL | 33.41 mL |
| 5 mM | 0.67 mL | 3.34 mL | 6.68 mL |
| 10 mM | 0.33 mL | 1.67 mL | 3.34 mL |
| 50 mM | 0.07 mL | 0.33 mL | 0.67 mL |
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References
References are publications that support the products' biological activity.
Bruns et al (1990) Structure-activity relationships for enhancement of adenosine A1 receptor binding by 2-amino-3-benzoylthiophenes. Mol.Pharmacol. 38 950 PMID: 2250667
Kollias-Baker et al (1997) Agonist-independent effect of an allosteric enhancer of the A1 adenosine receptor in CHO cells stably expressing the recombinant human A1 receptor. J.Pharmacol.Exp.Ther. 281 761 PMID: 9152383
Mizumura et al (1996) PD 81,723, an allosteric enhancer of the A1 adenosine receptor, lowers the threshold for ischemic preconditioning in dogs. Circ.Res. 79 415 PMID: 8781475
Musser et al (1999) Adenosine A1 receptor-dependent and -independent effects of the allosteric enhancer PD 81,723. J.Pharmacol.Exp.Ther. 288 446 PMID: 9918544
Keywords: PD 81723, supplier, Allosteric, potentiators, A1, receptors, Receptors, adenosines, PD81723, Adenosine, A1, Receptors, Adenosine, A1, Receptors, Tocris Bioscience
