PD 81723

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Cat.No. 1363 - PD 81723 | C14H12F3NOS | CAS No. 132861-87-1
Description: Allosteric potentiator of A1 receptors
Chemical Name: (2-Amino-4,5-dimethyl-3-thienyl)-[3-(trifluoromethyl)phenyl]methanone
Purity: ≥99% (HPLC)
Datasheet
Citations
Literature

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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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

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


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Keywords: PD 81723, supplier, Allosteric, potentiators, A1, receptors, Receptors, adenosines, PD81723, Adenosine, A1, Receptors, Adenosine, A1, Receptors, Tocris Bioscience

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