VU0357017
VU0357017 (CID-25010775) is a potent, selective and brain-penetrant allosteric agonist of M1 muscarinic acetylcholine receptor, with an EC50 of 477 nM. VU0357017 is highly selective for M1 and has no activity at M2-M5 up to the highest concentrations tested (30 μM). VU0357017 can be used for the research of Alzheimer’s disease and schizophrenia.
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- No. CAS: 1135681-23-0
- Fòrmula: C18H27N3O3
- Peso molecular:333.43
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
- Pureza y Documentación
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Help & FAQs
Actividad biológica
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
>30 μM
Compound: 8, ML071, VU0357017
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Agonist activity at rat muscarinic M2 receptor expressed in CHO cells
Agonist activity at rat muscarinic M2 receptor expressed in CHO cells
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[PMID: 21930376] |
| CHO | EC50 |
>30 μM
Compound: 8, ML071, VU0357017
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Agonist activity at rat muscarinic M3 receptor expressed in CHO cells
Agonist activity at rat muscarinic M3 receptor expressed in CHO cells
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[PMID: 21930376] |
| CHO | EC50 |
>30 μM
Compound: 8, ML071, VU0357017
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Agonist activity at rat muscarinic M4 receptor expressed in CHO cells
Agonist activity at rat muscarinic M4 receptor expressed in CHO cells
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[PMID: 21930376] |
| CHO | EC50 |
>30 μM
Compound: 8, ML071, VU0357017
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Agonist activity at rat muscarinic M5 receptor expressed in CHO cells
Agonist activity at rat muscarinic M5 receptor expressed in CHO cells
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[PMID: 21930376] |
| CHO | EC50 |
0.2 μM
Compound: 8, ML071, VU0357017
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Agonist activity at rat muscarinic M1 receptor expressed in CHO cells
Agonist activity at rat muscarinic M1 receptor expressed in CHO cells
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[PMID: 21930376] |
Chemical Information
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No. CAS 1135681-23-0
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Peso molecular 333.43
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Fòrmula C18H27N3O3
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SMILES
O=C(N1CCC(NCCNC(C2=CC=CC=C2C)=O)CC1)OCC
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Synonyms
CID-25010775 free base
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[1]. Digby GJ, et al. Chemical modification of the M(1) agonist VU0364572 reveals molecular switches in pharmacology and a bitopic binding mode. ACS Chem Neurosci. 2012 Dec 19;3(12):1025-36. [Content Brief]
[2]. Lebois EP, et al. Discovery and characterization of novel subtype-selective allosteric agonists for the investigation of M(1) receptor function in the central nervous system. ACS Chem Neurosci. 2010;1(2):104-121. [Content Brief]
[3]. Digby GJ, et al. Novel allosteric agonists of M1 muscarinic acetylcholine receptors induce brain region-specific responses that correspond with behavioral effects in animal models. J Neurosci. 2012 Jun 20;32(25):8532-44. [Content Brief]
[4]. Sheffler DJ, et al. Further exploration of M? allosteric agonists: subtle structural changes abolish M? allosteric agonism and result in pan-mAChR orthosteric antagonism. Bioorg Med Chem Lett. 2013 Jan 1;23(1):223-7. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
VU0357017 Related Classifications
HY-19752 Related Classifications
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