A positive allosteric modulator of adenosine A1 receptors
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VCP171

Item No. 30309

Technical Information
Formal Name
[2-amino-4-[3-(trifluoromethyl)phenyl]-3-thienyl]phenyl-methanone
CAS Number
1018830-99-3
Molecular Formula
C18H12F3NOS
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:6): 0.14 mg/mlEthanol: 10 mg/ml
λmax
210, 241 nm
SMILES
NC1=C(C(C2=CC=CC=C2)=O)C(C3=CC(C(F)(F)F)=CC=C3)=CS1
InChi Code
InChI=1S/C18H12F3NOS/c19-18(20,21)13-8-4-7-12(9-13)14-10-24-17(22)15(14)16(23)11-5-2-1-3-6-11/h1-10H,22H2
InChi Key
HNHLVOBHWXLIGP-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    Product Description

    VCP171 is a positive allosteric modulator of adenosine A1 receptors (EC50 = 15.8 μM in a kinetic assay measuring agonist dissociation).1. It reduces AMPA receptor-mediated evoked excitatory postsynaptic currents (eEPSCs) in lamina I and lamina II neurons in a rat model of neuropathic pain (EC50s = 1.995 and 0.251 μM, respectively) to a greater extent than in sham control animals (EC50s = 2.512 and 0.631 μM, respectively).2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Aurelio, L., Figler, H., Flynn, B.L., et al5-Substituted 2-aminothiophenes as A1 adenosine receptor allosteric enhancers. Bioorg. Med. Chem. 16(3), 1319-1327 (2008).

    2. Imlach, W.L., Bhola, R.F., May, L.T., et alA positive allosteric modulator of the adenosine A1 receptor selectively inhibits primary afferent synaptic transmission in a neuropathic pain model. Mol. Pharm. 88(3), 460-468 (2015).