1. GPCR/G Protein Neuronal Signaling
  2. mAChR
  3. VU0415248

VU0415248 is a selective muscarinic acetylcholine receptor 1 (M1) inhibitor. VU0415248 inhibits acetylcholine-induced calcium mobilization in cells expressing human and rat M1 muscarinic acetylcholine receptors, with an IC50 of 0.4 and 0.18 μM, respectively. VU0415248 is applicable to the research of Parkinson's disease, movement disorders and fragile X syndrome.

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VU0415248

VU0415248 Chemical Structure

CAS No. : 1359087-83-4

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Description

VU0415248 is a selective muscarinic acetylcholine receptor 1 (M1) inhibitor. VU0415248 inhibits acetylcholine-induced calcium mobilization in cells expressing human and rat M1 muscarinic acetylcholine receptors, with an IC50 of 0.4 and 0.18 μM, respectively. VU0415248 is applicable to the research of Parkinson's disease, movement disorders and fragile X syndrome[1].

IC50 & Target[1]

mAChR1

 

Cellular Effect
Cell Line Type Value Description References
CHO IC50
0.18 μM
Compound: 13l, VU0415248
Antagonist activity at rat muscarinic M1 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by fluorescence assay
Antagonist activity at rat muscarinic M1 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by fluorescence assay
[PMID: 22197142]
In Vitro

VU0415248 inhibits acetylcholine-induced calcium mobilization in human M1 muscarinic acetylcholine receptor-expressing cells with an IC50 of 0.4 μM[1].
VU0415248 (30 μM) inhibits acetylcholine-induced calcium mobilization in rat M1 muscarinic acetylcholine receptor-expressing cells with an IC50 of 0.18 μM, and shows very high selectivity over rat and human M2-5 muscarinic acetylcholine receptors (human M2-5 IC50 > 30 μM)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

425.50

Formula

C21H23N5O3S

CAS No.
SMILES

O=C(CCNS(=O)(C1=CC=CC2=NC=CC=C21)=O)N3CCN(CC3)C4=CC=NC=C4

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Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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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.

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VU0415248
Cat. No.:
HY-182587
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