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Submit ReviewLY 354740
Description: Potent and highly selective group II mGlu agonist
Chemical Name: (1S,2S,5R,6S)-2-Aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid
Purity: ≥98% (HPLC)
Biological Activity for LY 354740
LY 354740 is a highly selective and potent agonist of group II mGlu receptors (EC50 values are 5.1 and 24.3 nM at mGlu2 and mGlu3 receptors respectively and > 100000 nM at mGlu4, mGlu7, mGlu1a and mGlu5a receptors). Displays antianxiety and antiaddictive activity in vivo. Orally and systemically active.
Technical Data for LY 354740
| M. Wt | 185.18 |
| Formula | C8H11NO4 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 176199-48-7 |
| PubChem ID | 213056 |
| InChI Key | VTAARTQTOOYTES-RGDLXGNYSA-N |
| Smiles | N[C@]1([C@@](O)=O)[C@@]2([H])[C@@]([C@@H]2[C@](O)=O)([H])CC1 |
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.
Solubility Data for LY 354740
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| 1eq. NaOH | 18.52 | 100 |
Preparing Stock Solutions for LY 354740
The following data is based on the product molecular weight 185.18. Batch specific molecular weights may vary from batch to batch due to the degree 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 | 5.4 mL | 27 mL | 54 mL |
| 5 mM | 1.08 mL | 5.4 mL | 10.8 mL |
| 10 mM | 0.54 mL | 2.7 mL | 5.4 mL |
| 50 mM | 0.11 mL | 0.54 mL | 1.08 mL |
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Product Datasheets for LY 354740
References for LY 354740
References are publications that support the biological activity of the product.
Schoepp et al (1997) LY354740 is a potent and highly selective group II metabotropic glutamate receptor agonist in cell expressing human glutamate receptors. Neuropharmacology 36 1 PMID: 9144636
Helton et al (1998) Anxiolytic and side-effect profile of LY354740: a potent, highly selective, orally active agonist for group II metabotropic glutamate receptors. J.Pharmacol.Exp.Ther. 284 651 PMID: 9454811
Klodzinska et al (1999) Potential anti-anxiety, anti-addictive effects of LY 354740, a selective group II glutamate metabotropic receptors agonist in animal models. Neuropharmacology 38 1831 PMID: 10608278
If you know of a relevant reference for LY 354740, please let us know.
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Keywords: LY 354740, LY 354740 supplier, Potent, selective, group, II, mGlur, agonists, Group, Receptors, mGlu2, mGluR2, mGlu3, mGluR3, Glutamate, Metabotropic, LY354740, (Metabotropic), 3246, Tocris Bioscience
5 Citations for LY 354740
Citations are publications that use Tocris products. Selected citations for LY 354740 include:
Chai et al (2017) Neural Circuit-Specialized Astrocytes: Transcriptomic, Proteomic, Morphological, and Functional Evidence. Neuron 95 531 PMID: 28712653
Yaeger and Trussell (2015) Single granule cells excite Golgi cells and evoke feedback inhibition in the cochlear nucleus. J Neurosci 35 4741 PMID: 25788690
Scholler (2017) HTS-compatible FRET-based conformational sensors clarify membrane receptor activation. Nat Chem Biol 13 372 PMID: 28135236
Dornier (2017) Glutaminolysis drives membrane trafficking to promote invasiveness of breast cancer cells. Nat Commun 8 2255 PMID: 29269878
Copeland et al (2015) Neuronal activity patterns in the mediodorsal thalamus and related cognitive circuits are modulated by metabotropic glutamate receptors. Sci Rep 92 16 PMID: 25576798
Do you know of a great paper that uses LY 354740 from Tocris? Please let us know.
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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
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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