VCP 171

Pricing Availability   Qty
说明: Positive allosteric modulator (PAM) of A1 receptors; also allosteric partial agonist in absence of orthosteric agonist
化学名: [2-Amino-4-[3-(trifluoromethyl)phenyl]-3-thienyl]phenylmethanone
纯度: ≥98% (HPLC)
说明书
引用文献
评论

生物活性 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.

化合物库 for VCP 171

VCP 171 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。

技术数据 for VCP 171

分子量 347.35
公式 C18H12F3NOS
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 1018830-99-3
PubChem ID 24873485
InChI Key HNHLVOBHWXLIGP-UHFFFAOYSA-N
Smiles O=C(C1=C(N)SC=C1C2=CC(C(F)(F)F)=CC=C2)C3=CC=CC=C3

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for VCP 171

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 34.73 100
ethanol 34.73 100

制备储备液 for VCP 171

以下数据基于产品分子量 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.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 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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参考文献 for VCP 171

参考文献是支持产品生物活性的出版物。

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


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关键词: VCP 171, VCP 171 supplier, VCP171, Adensoisne, A1, receptors, positive, allosteric, modulators, partial, agonists, PAMs, Adenosine, Receptors, 6261, Tocris Bioscience

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