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AB141307

VU 0238429, allosteric M5 modulator

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(1 Publication)

MW 351.28 Da, Purity >99%. Selective, positive allosteric M5 modulator (EC50 values are 1.16 and >30 μM at M5 and M1/ M3 receptors, respectively). Shows no activity at M2 and M4 receptors.

View Alternative Names

7TM receptor, ACM2_HUMAN, ACM3_HUMAN, ACM4_HUMAN, ACM5_HUMAN, AChR, AChR M5, Acetylcholine receptor muscarinic 5, Acetylcholine receptor, muscarinic, 2, CHKM5MR, CHRM 2, CHRM 3, CHRM1, CM2, Cholinergic receptor muscarinic 1, Cholinergic receptor muscarinic 2, Cholinergic receptor muscarinic 4, Cholinergic receptor muscarinic 5, Cholinergic receptor, muscarinic 2, cardiac, Cholinergic receptor, muscarinic 2, isoform a, Cholinergic receptor, muscarinic 2a, Chrm 4, Chrm 5, EGBRS, FLJ43243, HM 2, HM 3, HM 4, HM 5, HM1, M2 muscarinic receptor, M2-mAChR, M3 muscarinic receptor, M4, M5R, MGC120006, MGC120007, MGC41838, Muscarinic M2 receptor, Muscarinic acetylcholine receptor M1, Muscarinic acetylcholine receptor M2, Muscarinic acetylcholine receptor M3, Muscarinic acetylcholine receptor M4, Muscarinic acetylcholine receptor M5, cholinergic receptor muscarinic 3, chrm2a, m3 muscarinic acetylcholine receptor, m5, muscarinic 3, muscarinic cholinergic m3 receptor, muscarinic m3 receptor

1 Images
Chemical Structure - VU 0238429, allosteric M5 modulator (AB141307)
  • Chemical Structure

Lab

Chemical Structure - VU 0238429, allosteric M5 modulator (AB141307)

2D chemical structure image of ab141307, VU 0238429, allosteric M5 modulator

Key facts

CAS number

1160247-92-6

Purity

>99%

Form

Solid

form

Molecular weight

351.28 Da

Molecular formula

C<sub>1</sub><sub>7</sub>H<sub>1</sub><sub>2</sub>F<sub>3</sub>NO<sub>4</sub>

PubChem

42633508

Nature

Synthetic

Solubility

Soluble in DMSO to 100 mM

Soluble in ethanol to 50 mM

Biochemical name

1-(4-Methoxybenzyl)-5-(trifluoromethoxy)indoline-2,3-dione

Biological description

Selective, positive allosteric M5 modulator (EC50 values are 1.16 and >30 μM at M5 and M1/ M3 receptors, respectively). Shows no activity at M2 and M4 receptors.

Canonical smiles

COC1=CC=C(C=C1)CN2C3=C(C=C(C=C3)OC(F)(F)F)C(=O)C2=O

InChi

InChI=1S/C17H12F3NO4/c1-24-11-4-2-10(3-5-11)9-21-14-7-6-12(25-17(18,19)20)8-13(14)15(22)16(21)23/h2-8H,9H2,1H3

InChiKey

CKLGZXFOLMHCMC-UHFFFAOYSA-N

IUPAC Name

1-[(4-methoxyphenyl)methyl]-5-(trifluoromethoxy)indole-2,3-dione

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Properties and storage information

Shipped at conditions
Ambient - Can Ship with Ice
Appropriate short-term storage conditions
+4°C
Appropriate long-term storage conditions
+4°C
Storage information
The product can be stored for up to 12 months
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Supplementary information

This supplementary information is collated from multiple sources and compiled automatically.

Muscarinic acetylcholine receptors also known as mAChRs are a group of G protein-coupled receptors that bind acetylcholine. They include five distinct subtypes: CHRM1 CHRM2 CHRM3 CHRM4 and CHRM5. These receptors have variable molecular masses ranging from approximately 50 to 60 kDa. Expression of muscarinic receptors is widespread present in both central and peripheral nervous systems and in non-neuronal tissues such as heart and smooth muscle. Each subtype has a unique pattern of distribution affecting how the body reacts to stimuli.
Biological function summary

Muscarinic receptors mediate parasympathetic nervous system responses. They do not function in isolation and may form complexes with other membrane proteins. mAChRs play roles in reducing heart rate constricting bronchi increasing secretions and modulating neurochemical activities in the central nervous system. Arecaidine can act as a muscarinic agonist whereas aclidinium serves as a muscarinic antagonist both influencing receptor activity through different pathways.

Pathways

Muscarinic receptors participate in the PI3K/AKT and MAPK signaling pathways. These pathways are key for cellular responses to environmental changes. For example muscarinic receptors in the cardiac tissue influence heart rate through these pathways interacting with proteins like Gi/o proteins. mAChRs also activate pathways involving other G protein receptors like adrenergic receptors to regulate vascular resistance and secretory processes.

Muscarinic receptors are linked to Alzheimer’s disease and chronic obstructive pulmonary disease (COPD). In Alzheimer’s imbalances in muscarinic receptor signaling can disrupt cognitive function. The CHRM1 subtype is particularly implicated in neurotransmission abnormalities associated with this disease. In COPD the CHRM3 subtype’s regulation of bronchoconstriction becomes clinically relevant. Therapeutic targeting of these receptors using antagonists like aclidinium helps manage symptoms and improve patient outcome.
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Product protocols

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Publications (1)

Recent publications for all applications. Explore the full list and refine your search

Neuroreport 32:577-582 PubMed33850081

2021

Protective effect of Houttuynia cordata extract on propofol-induced injury of rat hippocampal neurons by regulating PI3K/Akt and Toll-like receptor 4/NF-κB signaling pathway.

Applications

Unspecified application

Species

Unspecified reactive species

Hao Fang,Zhen Yang,Liu Yang
View all publications
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