VU 0357017 hydrochloride

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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)
Datasheet
Citations (3)
Reviews
Literature (2)

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.

Select a batch to recalculate based on the batch molecular weight:
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

Certificate of Analysis / Product Datasheet
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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:

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

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

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


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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


Alzheimer's Disease Poster

Alzheimer's Disease Poster

Alzheimer's disease (AD) is a debilitating and progressive neurodegenerative disease and the most common cause of dementia, affecting approximately 30% of individuals aged over 85 years. This poster summarizes the cellular and molecular mechanisms of AD.

Learning & Memory Poster

Learning & Memory Poster

Recognition memory enables us to make judgements about whether or not we have encountered a particular stimulus before. This poster outlines the cellular mechanisms underlying recognition memory and its links to long-term depression, as well as the use of pharmacological intervention to assess the role of neurotransmitters in recognition memory.