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

LY2794193 

Cat. No.: HY-119243 Purity: 99.88%
Handling Instructions

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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5 mg USD 550 In-stock
Estimated Time of Arrival: December 31
10 mg USD 850 In-stock
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50 mg USD 2850 In-stock
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100 mg USD 3950 In-stock
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Based on 1 publication(s) in Google Scholar

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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].

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].

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.

2173037-97-1

SMILES

O=C([[email protected]@]1(N)[[email protected]]2([H])[[email protected]@H](C(O)=O)[[email protected]]2([H])[[email protected]@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 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 3.33 mg/mL (9.96 mM; Need ultrasonic)

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
10 mM --- --- ---
*Please refer to the solubility information to select the appropriate solvent.
References

Purity: 99.88%

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Keywords:

LY2794193LY 2794193LY-2794193mGluRMetabotropic glutamate receptorsmGlu3painneurodegenerativediseasestraumaticbraininjuryInhibitorinhibitorinhibit

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Product name:
LY2794193
Cat. No.:
HY-119243
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