An M1 muscarinic acetylcholine receptor agonist
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VU0357017 (hydrochloride)

Item No. 11939

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[[2-[(2-methylbenzoyl)amino]ethyl]amino]-1-piperidinecarboxylic acid, ethyl ester, monohydrochloride
CAS Number
1135242-13-5
Synonyms
  • CID-25010775
Molecular Formula
C18H27N3O3 • HCl
Formula Weight
369.9
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 3 mg/mlPBS (pH 7.2): 5 mg/ml
SMILES
CC1=CC=CC=C1C(NCCNC2CCN(C(OCC)=O)CC2)=O.Cl
InChi Code
InChI=1S/C18H27N3O3.ClH/c1-3-24-18(23)21-12-8-15(9-13-21)19-10-11-20-17(22)16-7-5-4-6-14(16)2;/h4-7,15,19H,3,8-13H2,1-2H3,(H,20,22);1H
InChi Key
XKJQVUIXSBOCPP-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $28

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    5 mg

    $90

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    10 mg

    $165

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    25 mg

    $379

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    Product Description

    VU0357017 is an allosteric agonist of M1 muscarinic acetylcholine receptors (mAChRs; Ki = 9.91 µM in CHO cells).1 In vitro, it is selective for M1 over M2-M5 mAChRs (Kis = 21.4-50 µM in CHO cells). VU0357017 induces concentration-dependent increases in calcium mobilization and activates the ERK signaling pathway with EC50 values of 1.6 and 37 µM, respectively, in CHO cells expressing human recombinant M1 receptors.2 In vivo, VU0357017 crosses the blood-brain barrier and reverses scopolamine-induced deficits in contextual fear conditioning in rats when used at a dose of 10 mg/kg.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Digby, G.J., Utley, T.J., Lamsal, A., et al. Chemical modification of the M1 agonist VU0364572 reveals molecular switches in pharmacology and a bitopic binding mode. ACS Chem. Neurosci. 3(12), 1025-1036 (2012).

    2. Digby, G.J., Noetzel, M.J., Bubser, M., et al. Novel allosteric agonists of M1 muscarinic acetylcholine receptors induce brain region-specific responses that correspond with behavioral effects in animal models. J. Neurosci. 32(25), 8532-8544 (2012).

    3. Lebois, E.P., Bridges, T.M., Lewis, L.M., et al. 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(2), 104-121 (2010).