2. GPCR/G Protein Neuronal Signaling
  3. mAChR
  4. VU0476406

VU0476406 is a blood-brain barrier-permeable and selective muscarinic acetylcholine receptor subtype 4 (M4) activator with human EC50 of 91.0 nM and human pEC50 of 7.04. VU0476406 potentiates endogenous acetylcholine activity at M4 receptors. VU0476406 can be used for the research of Parkinson's disease.

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

VU0476406

VU0476406 Chemical Structure

CAS No. : 1451993-12-6

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VU0476406 Related Antibodies

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Description

VU0476406 is a blood-brain barrier-permeable and selective muscarinic acetylcholine receptor subtype 4 (M4) activator with human EC50 of 91.0 nM and human pEC50 of 7.04. VU0476406 potentiates endogenous acetylcholine activity at M4 receptors. VU0476406 can be used for the research of Parkinson's disease[1].

IC50 & Target[1]

mAChR4

91 nM (EC50)

mAChR4

7.04 (pEC50)

In Vitro

VU0476406 (Compound 8p) potently acts as a positive allosteric modulator of human M4 receptors in M4/Gqi5-CHO cells, with an EC50 of 91.0 nM and 74% acetylcholine maximum efficacy[1].
VU0476406 potently acts as a positive allosteric modulator of rat, dog, and cynomolgus monkey M4 receptors, with EC50 values of 13.5 nM, 111 nM, and 87.3 nM respectively[1].
VU0476406 is highly selective for M4 receptors, with no detectable activity (EC50 > 30 μM) at rat and human M1-3,5 receptors or dog and cynomolgus monkey M2 receptors[1].
VU0476406 has minimal inhibition of human CYP enzymes, with IC50 values ≥11 μM across tested CYP 1A2, 2C9, 2D6, and 3A4[1].
VU0476406 does not inhibit hERG channels, with an IC50 >33 μM[1].
VU0476406 (48 h) does not induce human CYP 1A2, 2B6, or 3A4 enzymes in cryopreserved human hepatocytes[1].

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

VU0476406 Related Antibodies
Parmacokinetics
Species Dose Route F
Rat[1] 10 mg/kg p.o. 54 %
Dog[1] 3 mg/kg p.o. 47 %
Cynomolgus Monkey[1] 10 mg/kg p.o. 4.7 %
In Vivo

VU0476406 (Compound 8p) (10 mg/kg; i.v.; single dose) significantly reduces dyskinesia scores and involuntary movements in non-human primates with L-DOPA (HY-N0304)-induced dyskinesia[1].
VU0476406 ameliorates deficits in synaptic plasticity and behavior in mice with L-DOPA-induced dyskinesia[1].
VU0476406 (10 mg/kg; p.o.; daily; 4 days) shows little to no auto-induction in Sprague-Dawley rats[1].

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

Animal Model: Cynomolgus monkey (non-human primate; L-DOPA-induced dyskinesia model)[1]
Dosage: 10 mg/kg
Administration: i.v.; single dose
Result: Significantly reduced dyskinesia scores and involuntary movements.
Animal Model: Sprague-Dawley rat[1]
Dosage: 10 mg/kg
Administration: p.o.; daily; 4 days
Result: Exhibited a day 4 versus day 1 AUC0-∞ ratio of 0.77, indicating little to no auto-induction in vivo.
Molecular Weight

407.46

Formula

C21H18FN5OS
CAS No.
SMILES

O=C(C1=C(N)C2=C(C)C(C)=NN=C2S1)NCC3=CC=C(C4=CC=CN=C4F)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.
Purity & Documentation
References
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VU0476406 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

VU04764061451993-12-6VU 0476406VU-0476406mAChRMuscarinic acetylcholine receptornon-human primatesMDCK-MDR1 cellsParkinson's disease modelsSprague-Dawley ratshERG channelsCYP enzymesmuscarinic acetylcholine receptor subtype 4L-DOPA-induced dyskinesiaM4/Gqi5-CHO cellsacetylcholineInhibitorinhibitorinhibit

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