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

VCP171 是一种有效的腺苷 A1 受体 (A1R) 正向变构调节剂。VCP171 能有效降低神经性疼痛模型 Lamina II 的兴奋性突触电流。VCP171 可用于神经性疼痛的研究。

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VCP171 Chemical Structure

VCP171 Chemical Structure

CAS No. : 1018830-99-3

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VCP171 相关抗体

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查看 Adenosine Receptor 亚型特异性产品:

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

  • 生物活性

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  • 参考文献

生物活性

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

 

细胞效力
(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]
体内研究
(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].

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.
分子量

347.35

Formula

C18H12F3NOS
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

VCP171 相关分类

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  • 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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目录号：
HY-113608
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