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VCP171 

Cat. No. M27646
VCP171  Structure
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Biological Activity

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.

Chemical Information
Molecular Weight 347.35
Formula C18H12F3NOS
CAS Number 1018830-99-3
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Giuseppe Deganutti, et al. J Chem Inf Model. Multisite Model of Allosterism for the Adenosine A1 Receptor

[2] Samantha L Cooper, et al. Br J Pharmacol. Probe dependence of allosteric enhancers on the binding affinity of adenosine A1 -receptor agonists at rat and human A1 -receptors measured using NanoBRET

[3] Yinglong Miao, et al. Sci Rep. Structural Basis for Binding of Allosteric Drυg Leads in the Adenosine A1 Receptor

[4] Anh T N Nguyen, et al. Mol Pharmacol. Role of the Second Extracellular Loop of the Adenosine A1 Receptor on Allosteric Modulator Binding, Signaling, and Cooperativity

[5] Wendy L Imlach, et al. Mol Pharmacol. A Positive Allosteric Modulator of the Adenosine A1 Receptor Selectively Inhibits Primary Afferent Synaptic Transmission in a Neuropathic Pain Model

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  Catalog
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Keywords: VCP171  supplier, Adenosine Receptor, inhibitors, activators


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