Biological Activity
Selective allosteric potentiator of M4 acetylcholine receptors (EC50 values are 33 and 0.7 nM for ACh in the absence and presence of VU10010 respectively). Binds to an allosteric site on the receptor increasing affinity for ACh and coupling to G-proteins.
Compound Libraries
VU 10010 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 345.85 |
| Formula | C17H16ClN3OS |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 633283-39-3 |
| PubChem ID | 714286 |
| InChI Key | FPRULFHDSFKYBV-UHFFFAOYSA-N |
| Smiles | CC1=C2C(SC(C(NCC3=CC=C(Cl)C=C3)=O)=C2N)=NC(C)=C1 |
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 | 34.59 | 100 | |
| ethanol | 3.46 | 10 |
Preparing Stock Solutions
The following data is based on the product molecular weight 345.85. 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 | 2.89 mL | 14.46 mL | 28.91 mL |
| 5 mM | 0.58 mL | 2.89 mL | 5.78 mL |
| 10 mM | 0.29 mL | 1.45 mL | 2.89 mL |
| 50 mM | 0.06 mL | 0.29 mL | 0.58 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Shirey et al (2008) An allosteric potentiator of M4 mAChR modulates hippocampal synaptic transmission. Nat.Chem.Biol. 4 42 PMID: 18059262
Keywords: VU 10010, supplier, Selective, allosteric, potentiator, M4, receptors, Muscarinic, Receptors, Acetylcholine, ACh, VU10010, M4, PAM, M4, Receptors, M4, Receptors, Tocris Bioscience
