1. GPCR/G Protein
    Neuronal Signaling
  2. mAChR
  3. VU10010

VU10010 

Cat. No.: HY-14563
Handling Instructions

VU10010 is a potent, highly selective and allosteric M4 mAChR potentiator with an EC50 of 400 nM. VU10010 binds to an allosteric site on M4 mAChR and increases affinity for acetylcholine and coupling to G proteins. VU10010 increases carbachol-induced depression of transmission at excitatory but not inhibitory synapses in the hippocampus.

For research use only. We do not sell to patients.

VU10010 Chemical Structure

VU10010 Chemical Structure

CAS No. : 633283-39-3

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Description

VU10010 is a potent, highly selective and allosteric M4 mAChR potentiator with an EC50 of 400 nM. VU10010 binds to an allosteric site on M4 mAChR and increases affinity for acetylcholine and coupling to G proteins. VU10010 increases carbachol-induced depression of transmission at excitatory but not inhibitory synapses in the hippocampus[1].

In Vitro

VU10010 potentiates the M4 response to acetylcholine 47-fold while having no activity at other mAChR subtypes (rM1, rM2, rM3 or rM5). VU10010 causes an increase in affinity for ACh and M4-mediated [35S]GTPγS binding[1].
VU10010 (10 μM) has no agonist, antagonist or allosteric potentiator activity at P2Y1R or mGluR5[1].
The EC50 values are 33 and 0.7 nM for ACh in the absence and presence of VU10010, respectively[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

345.85

Formula

C₁₇H₁₆ClN₃OS

CAS No.

633283-39-3

SMILES

O=C(C1=C(N)C2=C(C)C=C(C)N=C2S1)NCC3=CC=C(Cl)C=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

VU10010VU 10010VU-10010mAChRMuscarinic acetylcholine receptorallostericM4acetylcholineGproteinscarbacholdepressiontransmissionexcitatorysynapseshippocampusInhibitorinhibitorinhibit

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VU10010
Cat. No.:
HY-14563
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