YM 202074 sesquifumarate

Discontinued Product

YM 202074 sesquifumarate (Cat. No. 3413) has been withdrawn from sale for commercial reasons.
Description: High affinity, selective mGlu1 antagonist
Chemical Name: N-Cyclohexyl-6-[[N-(2-methoxyethyl)-N-methylamino]methyl]-N-methylthiazolo[3,2-a]benzoimidazole-2-carboxamide sesquifumarate
Purity: ≥99% (HPLC)
Literature (6)

Biological Activity for YM 202074 sesquifumarate

YM 202074 sesquifumarate is a high affinity, selective metabotropic glutamate receptor type 1 (mGlu1) antagonist. Binds an allosteric site of the rat mGlu1 receptor with a Ki of 4.8 nM. Inhibits mGlu1-mediated inositol phosphates production (IC50 = 8.6 nM in rat cerebellar granule cells). Neuroprotective in vivo.

Technical Data for YM 202074 sesquifumarate

M. Wt 588.67
Formula C22H30N4O2S.1.5C4H4O4
Storage Store at +4°C
Purity ≥99% (HPLC)
CAS Number 299900-84-8
PubChem ID 90488842
Smiles CN(CCOC)CC1=CC=C2C(N(C=C(C(N(C)C4CCCCC4)=O)S3)C3=N2)=C1.O=C(O)/C=C/C(O)=O.O=C(O)/C=C/C(O)=O.O=C(O)/C=C/C(O)=O.CN(CCOC)CC5=CC=C6C(N(C=C(C(N(C)C8CCCCC8)=O)S7)C7=N6)=C5

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Product Datasheets for YM 202074 sesquifumarate

References for YM 202074 sesquifumarate

References are publications that support the biological activity of the product.

Kohara et al (2008) Neuroprotective effects of the selective type 1 metabotropic glutamate receptor antagonist YM-202074 in rat stroke models. Brain Res. 1191 168 PMID: 18164695

Ferraguti et al (2008) Metabotropic glutamate 1 receptor: current concepts and perspectives. Pharmacol.Rev. 60 536 PMID: 19112153

Yanamoto et al (2010) Radiosynthesis and evaluation of [11C]YM-202074 as a PET ligand for imaging the metabotropic glutamate receptor type 1. Nucl.Med.Biol. 37 615 PMID: 20610166

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Citations for YM 202074 sesquifumarate

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Currently there are no citations for YM 202074 sesquifumarate.

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

Metabotropic Glutamate Receptors Scientific Review

Metabotropic Glutamate Receptors Scientific Review

Written by Francine Acher, this review discusses the pharmacology and therapeutic potential of mGlu receptors, and the compounds acting upon them; compounds available from Tocris are listed.

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