VCP 171

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Description: Positive allosteric modulator (PAM) of A1 receptors; also allosteric partial agonist in absence of orthosteric agonist
Chemical Name: [2-Amino-4-[3-(trifluoromethyl)phenyl]-3-thienyl]phenylmethanone
Purity: ≥98% (HPLC)

Biological Activity for VCP 171

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.

Compound Libraries for VCP 171

VCP 171 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for VCP 171

M. Wt 347.35
Formula C18H12F3NOS
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1018830-99-3
PubChem ID 24873485
Smiles O=C(C1=C(N)SC=C1C2=CC(C(F)(F)F)=CC=C2)C3=CC=CC=C3

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.

Solubility Data for VCP 171

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 34.73 100
ethanol 34.73 100

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 will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
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

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References for VCP 171

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

If you know of a relevant reference for VCP 171, please let us know.

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Citations for VCP 171

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