VU6077564
VU6077564 is a reversible competitive antagonist of M1 mAChR, with an IC50 of 31 nM in human (CHO cells) and 39.5 nM in rats. VU6077564 promotes axon growth of sensory neurons from adult rat dorsal root ganglia cultured in vitro. VU6077564 can be used for the research of peripheral neuropathy.
For research use only. We do not sell to patients.
- Formula: C26H27FN6O3S
- Molecular Weight:522.59
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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mAChR1 |
VU6077564 potently and selectively inhibits the human M1 muscarinic acetylcholine receptor in hM1-CHO cells, with an hM1 IC50 of 31 nM[1].
VU6077564 (10-point serial dilution curves) potently inhibits rat M1 muscarinic acetylcholine receptors, with an rM1 IC50 of 39.5 nM and an rM1 KB of 12 nM[1].
VU6077564 (0-1000 nM; 42 h) promotes axonal growth in cultured adult rat DRG sensory neurons, with an ED50 of 55 nM. It achieves a maximum 2-fold induction effect at 1000 nM without reducing neuronal viability[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | CLplasma | Vss | T1/2 (Elimination) |
|---|---|---|---|---|---|
| Rat[1] | 0.2 mg/kg | i.v. | 71.7 mL/min/kg | 27.6 L/kg | 35.2 h |
Chemical Information
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Molecular Weight 522.59
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Formula C26H27FN6O3S
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SMILES
O=S(C1=C2C=CC=NC2=C(F)C=C1)(N[C@H]3C[C@@H](C(N4[C@@H](C)CN(C5=NC(C)=C(C#N)C=C5)CC4)=O)C3)=O
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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)
- VU6077564
- VU 6077564
- VU-6077564
- mAChR
- peripheral neuropathy
- MDCKII-MDR1 P-gp
- P-glycoprotein
- hM1-CHO cells
- adult rat DRG sensory neurons
- human M1 muscarinic acetylcholine receptor
- adult rat dorsal root ganglia sensory neurons
- M1 mAChR
- central nervous system
- rat M1 muscarinic acetylcholine receptor
- Inhibitor
- inhibitor
- inhibit