2. GPCR/G Protein Neuronal Signaling
  3. mGluR
  4. LY2794193

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).

For research use only. We do not sell to patients.

LY2794193 Chemical Structure

LY2794193 Chemical Structure

CAS No. : 2173037-97-1

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10 mg USD 780 In-stock
50 mg USD 2500 In-stock
100 mg USD 3500 In-stock
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Based on 1 publication(s) in Google Scholar

LY2794193 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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)[1].

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].
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.

LY2794193 Related Antibodies
In Vivo

LY2794193 (1-30 mg/kg, s.c.), given 30 min prior to PCP (5 mg/kg, s.c.) leads a dose-related reduction in ambulations[1].
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.

Animal Model: Male Sprague-Dawley rats
Dosage: 1, 3, 10, or 30 mg/kg
Administration: Administrated s.c.; given 30 min prior to PCP (5 mg/kg, s.c.)
Result: A dose-related reduction in ambulations was observed, with the 10 and 30 mg/kg dose groups found to be statistically significant.
Molecular Weight

334.32

Formula

C16H18N2O6
CAS No.
Appearance

Solid

Color

White to off-white

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the 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.

* 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.

  • Protocol 1

    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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 5 mg/mL (14.96 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 98.16%

COA (256 KB) HNMR (379 KB) RP-HPLC (206 KB) LCMS (106 KB)

Handling Instructions (2659 KB)
References

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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LY2794193 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

LY27941932173037-97-1LY 2794193LY-2794193mGluRMetabotropic glutamate receptorsmGlu3painneurodegenerativediseasestraumaticbraininjuryInhibitorinhibitorinhibit

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