Product overview

Name VU 0357017 hydrochloride
Purity >98%
Description Potent, selective M1 receptor allosteric agonist
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Biological Data

Biological description Potent and selective M1 muscarinic receptor allosteric agonist (EC50 = 198 nM). Binds to the orthosteric ACh site at high concentrations to act as an antagonist. Reverses contextual fear conditioning deficits. Shows cognitive enhancing actions. Blood-brain barrier permeable.

Solubility & Handling

Storage instructions +4°C
Solubility overview Soluble in water (25mM) or DMSO (5mM)
Important This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use.

Calculators

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Dilution

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Chemical Data

Purity >98%
Chemical name 4-[[2-[(2-Methylbenzoyl)amino]ethyl ]amino]-1-piperidinecarboxylic acid ethyl ester hydrochloride
Molecular Weight 369.89
Chemical structure VU 0357017 hydrochloride  [1135242-13-5] Chemical Structure
Molecular Formula C18H27N3O3.HCl
CAS Number 1135242-13-5
PubChem identifier 25010775
SMILES CC1=CC=CC=C1C(NCCNC2CCN(C(OCC)=O)CC2)=O.Cl
InChiKey XKJQVUIXSBOCPP-UHFFFAOYSA-N

References for VU 0357017 hydrochloride

References are publications that support the biological activity of the product
  • Further exploration of M₁ allosteric agonists: subtle structural changes abolish M₁ allosteric agonism and result in pan-mAChR orthosteric antagonism.

    Sheffler DJ et al (2013) Bioorg Med Chem Lett 23(1) : 223-7.
  • Novel allosteric agonists of M1 muscarinic acetylcholine receptors induce brain region-specific responses that correspond with behavioral effects in animal models.

    Digby GJ et al (2012) J Neurosci 32(25) : 8532-44.
  • Discovery and characterization of novel subtype-selective allosteric agonists for the investigation of M(1) receptor function in the central nervous system.

    Lebois EP et al (2010) ACS Chem Neurosci 1(2) : 104-121.

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