2. GPCR/G Protein
  3. Adenosine Receptor
  4. VCP171

VCP171 is a potent adenosine A1 receptor (A1R) positive allosteric modulator (PAM). VCP171 is effective at decreasing excitatory synaptic currents in Lamina II of neuropathic pain model. VCP171 can be used for researching neuropathic pain.

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VCP171

VCP171 Chemical Structure

CAS No. : 1018830-99-3

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Based on 1 publication(s) in Google Scholar

VCP171 Related Antibodies

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Adenosine A1 receptor (A1R) Adenosine A2A receptor (A2AR) Adenosine A2B receptor (A2BR) Adenosine A3 receptor (A3R)

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Description

VCP171 is a potent adenosine A1 receptor (A1R) positive allosteric modulator (PAM). VCP171 is effective at decreasing excitatory synaptic currents in Lamina II of neuropathic pain model. VCP171 can be used for researching neuropathic pain[1].

IC50 & Target[1]

A1R

 

Cellular Effect
Cell Line Type Value Description References
CHO-K1 ED50
15.8 μM
Compound: 6b
Activity at human adenosine A1 receptor expressed in CHOK1 cells assessed as agonist-receptor ternary complex remaining by [35S]GTPgammaS binding assay
Activity at human adenosine A1 receptor expressed in CHOK1 cells assessed as agonist-receptor ternary complex remaining by [35S]GTPgammaS binding assay
[PMID: 17980606]
In Vivo

VCP171 (10 μM) reduces AMPAR-mediated evoked excitatory postsynaptic current (eEPSCs) in lamina I cells in sham and nerve-injured animals; increases paired pulse ration in cells from sham control animals; is significantly more effective in Lamina II neurons from nerve-injured animals than sham controls[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Neurons from male Sprague-Dawley rats (5-6 weeks; performed a partial nerve ligation (PNL) of the left sciatic nerve to create neuropathic pain model)[1]
Dosage: 10 μM
Administration: 0-30 min
Result: Reduced AMPAR-mediated evoked excitatory postsynaptic current (eEPSCs) in Lamina I cells in sham (13±2%, n=7 cells) and nerve-injured animals (24±4%, n=8 cells) compared with predrug controls; increased paired pulse ration in cells from sham control animals; was significantly more effective in Lamina II neurons from nerve-injured animals than sham controls.
Molecular Weight

347.35

Formula

C18H12F3NOS
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=C(N)SC=C1C2=CC(C(F)(F)F)=CC=C2)C3=CC=CC=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (287.89 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8789 mL 14.3947 mL 28.7894 mL
5 mM 0.5758 mL 2.8789 mL 5.7579 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8789 mL 14.3947 mL 28.7894 mL 71.9735 mL
5 mM 0.5758 mL 2.8789 mL 5.7579 mL 14.3947 mL
10 mM 0.2879 mL 1.4395 mL 2.8789 mL 7.1974 mL
15 mM 0.1919 mL 0.9596 mL 1.9193 mL 4.7982 mL
20 mM 0.1439 mL 0.7197 mL 1.4395 mL 3.5987 mL
25 mM 0.1152 mL 0.5758 mL 1.1516 mL 2.8789 mL
30 mM 0.0960 mL 0.4798 mL 0.9596 mL 2.3991 mL
40 mM 0.0720 mL 0.3599 mL 0.7197 mL 1.7993 mL
50 mM 0.0576 mL 0.2879 mL 0.5758 mL 1.4395 mL
60 mM 0.0480 mL 0.2399 mL 0.4798 mL 1.1996 mL
80 mM 0.0360 mL 0.1799 mL 0.3599 mL 0.8997 mL
100 mM 0.0288 mL 0.1439 mL 0.2879 mL 0.7197 mL
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VCP171 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

VCP1711018830-99-3VCP 171VCP-171Adenosine ReceptorP1 receptorA1Rneuropathic painLamina IIAMPARneuronsSprague-Dawley ratsInhibitorinhibitorinhibit

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