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Submit ReviewVU 0357017 hydrochloride
Description: Positive allosteric modulator of M1 receptors
Chemical Name: 4-[[2-[(2-Methylbenzoyl)amino]ethyl]amino]-1-piperidinecarboxylic acid ethyl ester hydrochloride
Purity: ≥98% (HPLC)
Biological Activity for VU 0357017 hydrochloride
VU 0357017 hydrochloride is a positive allosteric modulator of muscarinic M1 receptors (EC50 = 198 nM). Displays no activity at M2-M5 at concentrations up to 30 μM. Potentiates NMDA receptor currents in hippocampal neurons; activity reverses cognitive decifits in a rodent model of hippocampal-dependent memory. CNS penetrant.
Technical Data for VU 0357017 hydrochloride
| M. Wt | 369.89 |
| Formula | C18H27N3O3.HCl |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1135242-13-5 |
| PubChem ID | 25010775 |
| InChI Key | XKJQVUIXSBOCPP-UHFFFAOYSA-N |
| Smiles | CC1=CC=CC=C1C(NCCNC2CCN(C(OCC)=O)CC2)=O.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for VU 0357017 hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 9.25 | 25 | |
| DMSO | 1.85 | 5 |
Preparing Stock Solutions for VU 0357017 hydrochloride
The following data is based on the product molecular weight 369.89. 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.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.25 mM | 10.81 mL | 54.07 mL | 108.14 mL |
| 1.25 mM | 2.16 mL | 10.81 mL | 21.63 mL |
| 2.5 mM | 1.08 mL | 5.41 mL | 10.81 mL |
| 12.5 mM | 0.22 mL | 1.08 mL | 2.16 mL |
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Product Datasheets for VU 0357017 hydrochloride
References for VU 0357017 hydrochloride
References are publications that support the biological activity of the product.
Bridges et al (2010) Chemical lead optimization of a pan Gq mAChR M1, M3, M5 positive allosteric modulator (PAM) Lead. Part II. Development of potent and highly selective M1 PAM. Bioorg.Med.Chem.Lett. 20 1972 PMID: 20156687
Lebois et al (2010) Discovery and characterization of novel subtype-selective allosteric agonists for the investigation of M1 receptor function in the central nervous system. ACS Chem.Neurosci. 1 104
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Keywords: VU 0357017 hydrochloride, VU 0357017 hydrochloride supplier, VU0357017, hydrochloride, muscarinics, acetylcholine, machrs, positive, allosteric, modulators, pams, m1, selective, M1, Receptors, 4295, Tocris Bioscience
3 Citations for VU 0357017 hydrochloride
Citations are publications that use Tocris products. Selected citations for VU 0357017 hydrochloride include:
Jadeja et al (2016) Data regarding M1 muscarinic receptor-mediated modulation of hepatic catalase activity in response to oxidative stress. J Am Soc Nephrol 6 405 PMID: 26862589
Stefan et al (2018) Muscarinic M1 Receptor Overstimulation Disrupts Working Memory Activity for Rules in Primate Prefrontal Cortex. Neuron 98 1256-1268.e4 PMID: 29887340
Pasko et al (2020) Muscarinic M1 Receptors Modulate Working Memory Performance and Activity via KCNQ Potassium Channels in the Primate Prefrontal Cortex. Neuron 106 649-661.e4 PMID: 32197063
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