| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
LY-2794193 targets the metabotropic glutamate 3 (mGlu3) receptor, a G-protein coupled receptor that belongs to the group II metabotropic glutamate receptor family. It is a highly selective agonist with a Ki of 0.927 nM and an EC50 of 0.47 nM for human mGlu3. The compound exhibits 412 nM affinity (Ki) for mGlu2, demonstrating significant selectivity for mGlu3 over mGlu2.
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| ln Vitro |
In cultured paired cortical neurons, LY2794193 suppresses spontaneous Ca2+ oscillations with an EC50 of 43.6 nM[1]. With a combined maximal agonist efficacy (Emax) of 66%, LY2794193 demonstrates biphasic suppression of spontaneous Ca2+ transients in a coupled neuronal Ca2+ oscillation experiment (high affinity, EC50=0.44 nM; 48% of total agonist response; low affinity, EC50=43.6 nM; 52% of total agonist response) [1].
In vitro, LY-2794193 demonstrates highly potent and selective agonism at the mGlu3 receptor with a Ki of 0.927 nM and an EC50 of 0.47 nM. Its selectivity for mGlu3 over mGlu2 (Ki = 412 nM) is approximately 445-fold. By activating mGlu3 receptors, the compound modulates glutamatergic neurotransmission and downstream signaling pathways. |
| ln Vivo |
A dose-related decrease in walking is brought on by LY2794193 (1–30 mg/kg, subcutaneous injection), which is administered 30 minutes prior to PCP (5 mg/kg, subcutaneous injection) [1]. In cotton Sprague-Dawley, LY2794193 (1 mg/kg; iv) has an estimated half-life (T1/2) of 3.1 h, intermediate clearance (18.3 mL/min/kg), and SE (1.17 L/kg) [1]. LY2794193 (3 mg/kg; sc) produced an estimated bioavailability of 121% in the Sprague-Dawley, resulting in a quick shelf appearance (AUC=9.9 μM; Cmax=6.78 μM; Tmax=0.44 h) [1].
In vivo, LY-2794193 reduces akathisia seizures and depressive-like behaviors in rats. The compound increases GAT1, GLAST, and GLT-1 protein levels in rats. These effects suggest that mGlu3 receptor activation may enhance glutamate transporter expression and function, contributing to the compound's anticonvulsant and antidepressant-like effects. |
| Enzyme Assay |
In vitro receptor binding assays for mGlu3 agonism involve incubating membranes from cells expressing human recombinant mGlu3 or mGlu2 receptors with radiolabeled ligands (e.g., [³H]LY354740) and varying concentrations of LY-2794193. Functional assays measure the compound's ability to inhibit forskolin-stimulated cAMP accumulation in cells expressing mGlu3 or mGlu2 receptors, with EC50 values calculated from dose-response curves.
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| Cell Assay |
Cellular assays are performed using cell lines expressing human recombinant mGlu3 or mGlu2 receptors (e.g., CHO or HEK-293 cells). Cells are treated with LY-2794193 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 selectivity for mGlu3 over mGlu2 are determined by comparing EC50 values.
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| Animal Protocol |
Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rats
Doses: 1, 3, 10, or 30 mg/kg Route of Administration: subcutaneously (sc) (sc); subcutaneously (sc) (sc); 30 minutes before PCP (5 mg/kg, subcutaneously (sc) (sc)) Experimental Results: Observed and Dose There was an associated reduction in activity that was statistically significant at the 10 and 30 mg/kg doses. In vivo studies are conducted in rat models of seizures and depression. LY-2794193 is administered intraperitoneally or orally at various doses. Seizure activity is assessed in the akathisia seizure model. Depressive-like behaviors are evaluated using the forced swim test or tail suspension test. Brain tissue is collected for Western blot analysis of GAT1, GLAST, and GLT-1 protein levels. |
| ADME/Pharmacokinetics |
LY-2794193 (molecular weight 334.32, formula C₁₆H₁₈N₂O₆) 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 LY-2794193 in animal models. As an mGlu3 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 for studying mGlu3 receptor function.
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| References | |
| Additional Infomation |
LY-2794193 is a highly potent and selective mGlu3 receptor agonist developed as a research tool for studying mGlu3 receptor function. Its mechanism involves selective activation of mGlu3 receptors, modulating glutamatergic neurotransmission and downstream signaling pathways. The compound has demonstrated anticonvulsant and antidepressant-like effects in preclinical models. LY-2794193 is primarily used for research purposes and has not received regulatory approval for clinical use.
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| Molecular Formula |
C16H18N2O6
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|---|---|
| Molecular Weight |
334.323924541473
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| Exact Mass |
334.116
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| CAS # |
2173037-97-1
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| PubChem CID |
60096231
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| Appearance |
White to off-white solid powder
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| LogP |
-2.6
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
24
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| Complexity |
567
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| Defined Atom Stereocenter Count |
5
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| SMILES |
OC([C@H]1[C@@H]2[C@H](C[C@@](C(=O)O)([C@@H]21)N)NC(C1C=CC=C(C=1)OC)=O)=O
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| InChi Key |
UXNRHIJPZNNDDJ-VZAVHYRXSA-N
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| InChi Code |
InChI=1S/C16H18N2O6/c1-24-8-4-2-3-7(5-8)13(19)18-9-6-16(17,15(22)23)12-10(9)11(12)14(20)21/h2-5,9-12H,6,17H2,1H3,(H,18,19)(H,20,21)(H,22,23)/t9-,10-,11-,12-,16-/m0/s1
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| Chemical Name |
(1S,2S,4S,5R,6S)-2-Amino-4-[(3-methoxybenzoyl)amino]bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
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| Synonyms |
LY2794193; LY-2794193; LY 2794193
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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 |
| 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) |
DMSO : ~200 mg/mL (~598.23 mM)
H2O : ~2 mg/mL (~5.98 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (14.96 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 5 mg/mL (14.96 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9911 mL | 14.9557 mL | 29.9115 mL | |
| 5 mM | 0.5982 mL | 2.9911 mL | 5.9823 mL | |
| 10 mM | 0.2991 mL | 1.4956 mL | 2.9911 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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