VU0357017 (Synonyms: CID-25010775 free base)

Cat. No.: HY-19752: Data Sheet Handling Instructions
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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.

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

VU0357017 Chemical Structure

CAS No. : 1135681-23-0

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This product is a controlled substance and not for sale in your territory.

Other In-stock Forms of VU0357017:

VU0357017 hydrochloride

Other Forms of VU0357017:

VU0357017 hydrochloride In-stock

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•Related Small Molecules:

•Related Proteins:

View All mAChR Isoform Specific Products:

View All Isoforms

mAChR1 mAChR2 mAChR3 mAChR4 mAChR5

Biological Activity
Purity & Documentation
References
Customer Review

Description

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	0.2 μM Compound: 8, ML071, VU0357017	Agonist activity at rat muscarinic M1 receptor expressed in CHO cells Agonist activity at rat muscarinic M1 receptor expressed in CHO cells	[PMID: 21930376]
CHO	EC₅₀	> 30 μM Compound: 8, ML071, VU0357017	Agonist activity at rat muscarinic M2 receptor expressed in CHO cells Agonist activity at rat muscarinic M2 receptor expressed in CHO cells	[PMID: 21930376]
CHO	EC₅₀	> 30 μM Compound: 8, ML071, VU0357017	Agonist activity at rat muscarinic M3 receptor expressed in CHO cells Agonist activity at rat muscarinic M3 receptor expressed in CHO cells	[PMID: 21930376]
CHO	EC₅₀	> 30 μM Compound: 8, ML071, VU0357017	Agonist activity at rat muscarinic M4 receptor expressed in CHO cells Agonist activity at rat muscarinic M4 receptor expressed in CHO cells	[PMID: 21930376]
CHO	EC₅₀	> 30 μM Compound: 8, ML071, VU0357017	Agonist activity at rat muscarinic M5 receptor expressed in CHO cells Agonist activity at rat muscarinic M5 receptor expressed in CHO cells	[PMID: 21930376]

Molecular Weight

333.43

Formula

C₁₈H₂₇N₃O₃

CAS No.

1135681-23-0

SMILES

O=C(N1CCC(NCCNC(C2=CC=CC=C2C)=O)CC1)OCC

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

Handling Instructions (2659 KB)

References

[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]

VU0357017 Related Classifications

Neurological Disease

Molarity Calculator
Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass		Concentration		Volume		Molecular Weight *
	=		×		×

The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)	×	Volume _(start)	=	Concentration _(final)	×	Volume _(final)
	×		=		×
C1		V1		C2		V2

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:

VU03570171135681-23-0CID-25010775VU 0357017VU-0357017CID25010775CID 25010775mAChRMuscarinic acetylcholine receptorM1Rα-syncognitive impairmentInhibitorinhibitorinhibit

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