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VCP 171 is an adenosine A1 receptor positive allosteric modulator (PAM) (pKB = 5.65, binding cooperativity with NECA 0.68). In absence of orthosteric agonist, VCP171 behaves as an allosteric partial agonist, inhibiting cAMP activity. Inhibits AMPA receptor-mediated evoked excitatory postsynaptic current (eEPSC) amplitude in lamina I and II neurons in a rat partial nerve-injury model of neuropathic pain.
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|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
The following data is based on the product molecular weight 347.35. 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.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.88 mL||14.39 mL||28.79 mL|
|5 mM||0.58 mL||2.88 mL||5.76 mL|
|10 mM||0.29 mL||1.44 mL||2.88 mL|
|50 mM||0.06 mL||0.29 mL||0.58 mL|
References are publications that support the biological activity of the product.
Christopoulos et al (2016) Role of the second extracellular loop of the adenosine A1 receptor on allosteric modulator binding, signaling, and cooperativity. Mol.Pharmacol. 90 715 PMID: 27683013
Imlach et al (2015) A positive allosteric modulator of the adenosine A1 receptor selectively inhibits primary afferent synaptic transmission in a neuropathic pain model. Mol.Pharmacol. 88 460 PMID: 26104547
Aurelio et al (2008) 5-Substituted 2-aminothiophenes as A1 adenosine receptor allosteric enhancers. Bioorg.Med.Chem. 16 1319 PMID: 17980606
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Keywords: VCP 171, VCP 171 supplier, VCP171, Adensoisne, A1, receptors, positive, allosteric, modulators, partial, agonists, PAMs, Adenosine, Receptors, 6261, Tocris Bioscience
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