Biological Activity
Type II positive allosteric modulator of α7 nACh receptors (pEC50 = 5.5). Displays no agonist activity at α7 receptors at concentrations up to 0.1 mM; potentiates agonist-evoked responses and reduces rate of desensitization of α7 nAChRs. Exhibits potency and efficacy similar to PNU 120596 (Cat. No. 2498).
Technical Data
| M. Wt | 376.47 |
| Formula | C22H20N2O2S |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 353483-92-8 |
| PubChem ID | 5038679 |
| InChI Key | SIZWDJIHABLBSP-UHFFFAOYSA-N |
| Smiles | O=S(C3=CC1=C(C=C3)NC(C4=C(C=CC=C5)C5=CC=C4)C2C1C=CC2)(N)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 18.82 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 376.47. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.66 mL | 13.28 mL | 26.56 mL |
| 5 mM | 0.53 mL | 2.66 mL | 5.31 mL |
| 10 mM | 0.27 mL | 1.33 mL | 2.66 mL |
| 50 mM | 0.05 mL | 0.27 mL | 0.53 mL |
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References
References are publications that support the products' biological activity.
Gronlien et al (2007) Distinct profiles of α7 nAChR positive allosteric modulation revealed by structurally diverse chemotypes. Mol.Pharmacol. 72 715 PMID: 17565004
Gill et al (2011) Agonist activation of α7 nicotinic acetylcholine receptors via an allosteric transmembrane site. Proc.Natl.Acad.Sci. 108 5867 PMID:
Keywords: TQS, supplier, positive, allosteric, modulators, pam, alpha, α, a7, nicotinic, receptors, nachr, type, II, Nicotinic, (a7), Receptors, Nicotinic, (a7), Receptors, Tocris Bioscience
