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.
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- CAS No.: 1451993-12-6
- Formule: C21H18FN5OS
- Masse moléculaire:407.46
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
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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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Masse moléculaire 407.46
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
VU0476406 Related Classifications
HY-183203 Related Classifications
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