VCP 171

Product Description

VCP 171 is an adenosine A₁ receptor positive allosteric modulator (PAM) (pK_B = 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.

Solubility

Preparing Stock Solutions for VCP 171

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 all affect the solvent volumes required to prepare stock solutions.

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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

Calculators

Background References

References are publications that support the biological activity of the product.

• Imlach A positive allosteric modulator of the adenosine A₁ receptor selectively inhibits primary afferent synaptic transmission in a neuropathic pain model. Mol.Pharmacol. 2015 PMID: 26104547
• Aurelio 5-Substituted 2-aminothiophenes as A₁ adenosine receptor allosteric enhancers. Bioorg.Med.Chem. 2008 PMID: 17980606
• Christopoulos Role of the second extracellular loop of the adenosine A₁ receptor on allosteric modulator binding, signaling, and cooperativity. Mol.Pharmacol. 2016 PMID: 27683013