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.
- CAS No.: 1451993-12-6
- Formula: C21H18FN5OS
- Molecular Weight:407.46
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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Biological Activity
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mAChR4 91 nM (EC50) |
mAChR4 7.04 (pEC50) |
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 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.
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Animal Model:Cynomolgus monkey (non-human primate; L-DOPA-induced dyskinesia model)[1]
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Dosage:10 mg/kg
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Administration:i.v.; single dose
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Result:Significantly reduced dyskinesia scores and involuntary movements.
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Animal Model:Sprague-Dawley rat[1]
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Dosage:10 mg/kg
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Administration:p.o.; daily; 4 days
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Result:Exhibited a day 4 versus day 1 AUC0-∞ ratio of 0.77, indicating little to no auto-induction in vivo.
Chemical Information
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CAS No. 1451993-12-6
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Molecular Weight 407.46
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Formula C21H18FN5OS
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SMILES
O=C(C1=C(N)C2=C(C)C(C)=NN=C2S1)NCC3=CC=C(C4=CC=CN=C4F)C=C3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
VU0476406 Related Classifications
HY-183203 Related Classifications
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