| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
LY2812223 targets the metabotropic glutamate 2 (mGlu2) receptor, a G-protein coupled receptor belonging to the group II metabotropic glutamate receptor family. It is a functionally selective agonist with binding affinity (Ki) of 144 nM for mGlu2 and 156 nM for mGlu3. By activating mGlu2 receptors, the compound modulates glutamatergic neurotransmission and downstream signaling pathways.
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| ln Vitro |
In vitro, LY2812223 demonstrates potent binding affinity for mGlu2 (Ki = 144 nM) and mGlu3 (Ki = 156 nM). The compound's functional selectivity for mGlu2 over mGlu3 distinguishes it from LY354740, which was a dual agonist. By selectively activating mGlu2 receptors, LY2812223 allows for more precise modulation of mGlu2-mediated signaling pathways.
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| ln Vivo |
In vivo, LY2812223 has been evaluated in preclinical models to study the role of mGlu2 receptors in various neurological and psychiatric conditions. As a functionally selective mGlu2 agonist, it has been used to investigate the therapeutic potential of mGlu2 activation in anxiety, schizophrenia, and other disorders.
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| Enzyme Assay |
In vitro receptor binding assays for mGlu2/3 agonism involve incubating membranes from cells expressing human recombinant mGlu2 or mGlu3 receptors with radiolabeled ligands (e.g., [³H]LY354740) and varying concentrations of LY2812223. Functional assays measure the compound's ability to inhibit forskolin-stimulated cAMP accumulation in cells expressing mGlu2 or mGlu3 receptors. Ki values are calculated from competition binding curves.
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| Cell Assay |
Cellular assays are performed using cell lines expressing human recombinant mGlu2 or mGlu3 receptors (e.g., CHO or HEK-293 cells). Cells are treated with LY2812223 at various concentrations in the presence of forskolin. Intracellular cAMP levels are measured using a luminescent or fluorescent cAMP detection kit. The compound's potency and functional selectivity for mGlu2 over mGlu3 are determined by comparing EC50 or Ki values.
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| Animal Protocol |
In vivo studies are conducted in rodent models of psychiatric and neurological disorders. LY2812223 is administered intraperitoneally or orally at various doses. Behavioral tests such as the prepulse inhibition test, elevated plus maze, or forced swim test are performed to assess the compound's effects on sensorimotor gating, anxiety, and depression-like behaviors. Brain tissue is collected for biomarker analysis.
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| ADME/Pharmacokinetics |
LY2812223 (molecular weight 372.37, formula C₁₉H₂₄N₂O₆) is a small-molecule compound. It is soluble in DMSO and is typically stored at -20°C. Its physicochemical properties support its use in both in vitro and in vivo studies.
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| Toxicity/Toxicokinetics |
Preclinical toxicity studies have evaluated LY2812223 in animal models. As an mGlu2 receptor agonist, its toxicity profile is related to modulation of glutamatergic neurotransmission. No significant toxicity has been reported at therapeutic doses. The compound's safety profile supports its use in research applications.
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| References | |
| Additional Infomation |
LY2812223 is a functionally selective mGlu2 receptor agonist derived from research on LY354740. Its mechanism involves selective activation of mGlu2 receptors, modulating glutamatergic neurotransmission. The compound exhibits binding affinity (Ki) of 144 nM for mGlu2 and 156 nM for mGlu3. LY2812223 is primarily used as a research tool to study mGlu2 receptor function and has not received regulatory approval for clinical use.
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| Molecular Formula |
C10H12N4O4S
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|---|---|
| Molecular Weight |
284.291680335999
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| Exact Mass |
284.057
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| CAS # |
1311385-20-2
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| PubChem CID |
53240406
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| Appearance |
White to off-white solid powder
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| LogP |
-2.9
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
19
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| Complexity |
436
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| Defined Atom Stereocenter Count |
5
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| SMILES |
S(C1=NC=NN1)[C@@H]1C[C@@](C(=O)O)([C@@H]2[C@@H](C(=O)O)[C@@H]21)N
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| InChi Key |
YSOWRGMLMZQSBX-AVUIYAGVSA-N
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| InChi Code |
InChI=1S/C10H12N4O4S/c11-10(8(17)18)1-3(19-9-12-2-13-14-9)4-5(6(4)10)7(15)16/h2-6H,1,11H2,(H,15,16)(H,17,18)(H,12,13,14)/t3-,4+,5+,6+,10+/m1/s1
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| Chemical Name |
(1S,2S,4R,5R,6S)-2-Amino-4-methylbicyclo[3.1.0]hexane2,6-dicarboxylic acidLY-2812223; (1R,2S,4R,5R,6R)-2-Amino-4-(1H-1,2,4-triazol-3-ylsulfanyl)bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
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| Synonyms |
LY-2812223; LY 2812223; LY2812223
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ~50 mg/mL (~175.88 mM)
DMSO : ~28.75 mg/mL (~101.13 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 140 mg/mL (492.45 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.5175 mL | 17.5877 mL | 35.1753 mL | |
| 5 mM | 0.7035 mL | 3.5175 mL | 7.0351 mL | |
| 10 mM | 0.3518 mL | 1.7588 mL | 3.5175 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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