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Submit ReviewPD 81723 is an 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.
分子量 | 299.31 |
公式 | C14H12F3NOS |
储存 | Store at RT |
纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
ethanol | 29.93 | 100 | |
DMSO | 29.93 | 100 |
以下数据基于产品分子量 299.31。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 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 |
参考文献是支持产品生物活性的出版物。
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
If you know of a relevant reference for PD 81723, please let us know.
关键词: PD 81723, PD 81723 supplier, Allosteric, potentiators, A1, receptors, Receptors, adenosines, PD81723, Adenosine, 1363, Tocris Bioscience
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