索取文献 | Tocris 生物科学,Tocris/PD 81723/1363/50/50 mg-蚂蚁淘生物

Description: Allosteric potentiator of A₁ receptors Chemical Name: (2-Amino-4,5-dimethyl-3-thienyl)-[3-(trifluoromethyl)phenyl]methanone Purity: ≥99% (HPLC) Biological Activity Technical Data Solubility Calculators DatasheetsReferences

Biological Activity

Allosteric potentiator at the adenosine A₁ receptor; acts via agonist-dependent and -independent mechanisms. Enhances agonist affinity for, and increased t_½ 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 Safety Datasheet Select another language: English German French Spanish View SDS

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