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4BP-TQS

Cat. No. M8461

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4BP-TQS Structure

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Biological Activity

4BP-TQS is an atypical agonist of a7-nAChR that binds to the receptor in an intrasubunit cavity, and activates the channel via a mechanism that is distinct from conventional agonists. Maximal activation of a7-nAChR by 4BP-TQS is eight fold greater than activation by a maximum dose of acetylcholine (Ach), and 4BP-TQS can poteniate an EC10 concentration of ACh to invoke a response that is 540-fold higher than the maximal dose of ACh alone.

Chemical Information
Molecular Weight 405.31
Formula C18H17BrN2O2S
CAS Number 360791-49-7
Solubility (25°C) DMSO: 20 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Roger L Papke, et al. Differing Activity Profiles of the Stereoisomers of 2,3,5,6TMP-TQS, a Putative Silent Allosteric Modulator of α 7 nAChR

[2] Ganesh A Thakur, et al. Expeditious synthesis, enantiomeric resolution, and enantiomer functional characterization of (4-(4-bromophenyl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-8-sulfonamide (4BP-TQS): an allosteric agonist-positive allosteric modulator of α7 nicotinic ac䲧畸Ỵ畹㧀畷羹皖

[3] Magda M Pałczyńska, et al. Activation of α7 nicotinic receptors by orthosteric and allosteric agonists: influence on single-channel kinetics and conductance

[4] JasKiran K Gill, et al. A series of α7 nicotinic acetylcholine receptor allosteric modulators with close chemical similarity but diverse pharmacological properties

[5] Jaskiran K Gill, et al. Agonist activation of alpha7 nicotinic acetylcholine receptors via an allosteric transmembrane site

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Keywords: 4BP-TQS supplier, inhibitors, activators

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