Chemical Name: 4-(Cycloheptylamino)-N-[[(2R)-tetrahydro-2-furanyl]methyl]-thieno[2,3-d]pyrimidine-6-methanamine
Purity: ≥99% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
Biological Activity
Selective mGlu1 antagonist (Ki = 13 nM). Inhibits mGlu1-mediated inositol phosphate production in rat cerebellar granule cells (IC50 = 13 nM). Displays antinociceptive and analgesic effects in vitro; exhibits no significant sedative effect on locomotor activity.
Licensing Information
Sold with the permission of Astellas Pharma Inc.
Technical Data
M. Wt
360.52
Formula
C19H28N4OS
Storage
Store at RT
Purity
≥99% (HPLC)
CAS Number
446257-23-4
PubChem ID
11682007
InChI Key
SASNRPJKZVJWQW-OAHLLOKOSA-N
Smiles
C1(NC4CCCCCC4)=C(C=C(CNC[C@H]3CCCO3)S2)C2=NC=N1
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solvent
Max Conc. mg/mL
Max Conc. mM
Solubility
DMSO
36.05
100
ethanol
36.05
100
Preparing Stock Solutions
The following data is based on the product molecular weight 360.52. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass
1 mg
5 mg
10 mg
1 mM
2.77 mL
13.87 mL
27.74 mL
5 mM
0.55 mL
2.77 mL
5.55 mL
10 mM
0.28 mL
1.39 mL
2.77 mL
50 mM
0.06 mL
0.28 mL
0.55 mL
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Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Koharaet al (2007) Antinociceptive profile of a selective metabotropic glutamate receptor 1 antagonist YM-230888 in chronic pain rodent models. Eur.J.Pharmacol. 571 8 PMID: 17597604
Satowet al (2008) Pharmacological effects of the metabotropic glutamate receptor 1 antagonist compared with those of the metabotropic glutamate receptor 5 antagonist and metabotropic glutamate receptor 2/3 agonist in rodents: detailed investigations with a selective allost J.Pharmacol.Exp.Ther. 326 577 PMID: 18487514
Keywords: YM 230888, supplier, YM230888, mGlu1, metabotropic, glutamate, receptors, group, I, 1, antagonist, antagonists, mGlu, selective, Glutamate, (Metabotropic), Group, I, Receptors, Glutamate, (Metabotropic), Group, I, Receptors, Tocris Bioscience