LY2794193
Based on 1 publication(s) in Google Scholar
LY2794193 is a highly potent and selective mGlu3 receptor agonist (hmGlu3 Ki=0.927 nM，EC50=0.47 nM; hmGlu2 Ki=412 nM，EC50=47.5 nM).
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- Pureté : 99.65%
- CAS No.: 2173037-97-1
- Formule: C16H18N2O6
- Masse moléculaire:334.32
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) LY2794193
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Activité biologique
Description
IC50 & Target
[1]|
mGluR3 0.47 nM (EC50) |
mGluR3 0.927 nM (Ki) |
mGluR2 47.5 (EC50) |
mGluR2 412 (Ki) |
In Vitro
LY2794193 exhihits inhibition of spontaneous Ca2+ oscillations in cultured rat cortical neurons with an EC50 of 43.6 nM[1].
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In the rat cortical neuron Ca2+ oscillation assay, LY2794193 exhibits a biphasic inhibition of spontaneous Ca2+ transients (high affinity EC50=0.44 nM; 48% of the total agonist response; low affinity EC50=43.6 nM; 52% of the total agonist response) with combined maximal agonist efficacy (Emax) of 66%[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
In Vivo
? LY2794193 (1 mg/kg; i.v.) exhibits moderate clearance (18.3 mL/min per kg) and volume of distribution (1.17 L/kg) with a calculated plasma half-life (T1/2) of 3.1 h in Male Sprague-Dawley rats[1].
? LY2794193 (3 mg/kg; s.c.) leads to the rapid appearance in the plasma (AUC=9.9 μM; Cmax=6.78 μM; Tmax=0.44 h) and a calculated bioavailability of 121% in male Sprague-Dawley rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats
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Dosage:1, 3, 10, or 30 mg/kg
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Administration:Administrated s.c.; given 30 min prior to PCP (5 mg/kg, s.c.)
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Result:A dose-related reduction in ambulations was observed, with the 10 and 30 mg/kg dose groups found to be statistically significant.
Chemical Information
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CAS No. 2173037-97-1
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Appearance Solid
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Masse moléculaire 334.32
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Formule C16H18N2O6
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Color White to off-white
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SMILES
O=C([C@@]1(N)[C@]2([H])[C@@H](C(O)=O)[C@]2([H])[C@@H](NC(C3=CC=CC(OC)=C3)=O)C1)O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Cell Res
2025 Mar;35(3):165-185. PMID: 39875551
Solvant et solubilité
In Vitro:
DMSO : 200 mg/mL (598.23 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 2 mg/mL (5.98 mM; ultrasonic and adjust pH to 14 with NaOH)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (14.96 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (279 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.9911 mL | 14.9557 mL | 29.9115 mL | 74.7787 mL |
| 5 mM | 0.5982 mL | 2.9911 mL | 5.9823 mL | 14.9557 mL | |
| DMSO | 10 mM | 0.2991 mL | 1.4956 mL | 2.9911 mL | 7.4779 mL |
| 15 mM | 0.1994 mL | 0.9970 mL | 1.9941 mL | 4.9852 mL | |
| 20 mM | 0.1496 mL | 0.7478 mL | 1.4956 mL | 3.7389 mL | |
| 25 mM | 0.1196 mL | 0.5982 mL | 1.1965 mL | 2.9911 mL | |
| 30 mM | 0.0997 mL | 0.4985 mL | 0.9970 mL | 2.4926 mL | |
| 40 mM | 0.0748 mL | 0.3739 mL | 0.7478 mL | 1.8695 mL | |
| 50 mM | 0.0598 mL | 0.2991 mL | 0.5982 mL | 1.4956 mL | |
| 60 mM | 0.0499 mL | 0.2493 mL | 0.4985 mL | 1.2463 mL | |
| 80 mM | 0.0374 mL | 0.1869 mL | 0.3739 mL | 0.9347 mL | |
| 100 mM | 0.0299 mL | 0.1496 mL | 0.2991 mL | 0.7478 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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