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LY-487379

Cat No.:V50233 Purity: ≥98%
LY487379 is a selective human mGluR2 positive allosteric modulator (PAM).
LY-487379
LY-487379 Chemical Structure CAS No.: 353231-17-1
Product category: New3
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
50mg
100mg
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Other Forms of LY-487379:

  • LY487379 HCl
Official Supplier of:
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Top Publications Citing lnvivochem Products
Product Description
LY487379 is a selective human mGluR2 positive allosteric modulator (PAM). LY487379 enhances glutamate-stimulated [35S]GTPγS binding to mGlu2 and mGlu3 receptors with EC50s of 1.7 μM and >10 μM, respectively. LY487379 promotes cognitive flexibility and behavioral inhibition in rats. LY487379 may be used in schizophrenia research.
Biological Activity I Assay Protocols (From Reference)
ln Vivo
LY487379 (ip; 30 mg/kg; injected 30 min before testing) required significantly fewer trials to meet criteria during the ED phase of the ASST in the attention-shift task in male Sprague-Dawley rats. But there is no clear pharmacological impact in any other discrimination stage [1]. LY487379 hydrochloride (ip; 10-30 mg/kg) generated a rise in microdialysate norepinephrine levels; the dose response was bell-shaped. It dose-dependently enhances extracellular serotonin levels in the medial prefrontal cortex of male Sprague-Dawley rats [1].
References
[1]. Nikiforuk A, et al. Effects of a positive allosteric modulator of group II metabotropic glutamate receptors, LY487379, on cognitive flexibility and impulsive-like responding in rats. J Pharmacol Exp Ther. 2010;335(3):665-673.
[2]. Schaffhauser H, et al. Pharmacological characterization and identification of amino acids involved in the positive modulation of metabotropic glutamate receptor subtype 2. Mol Pharmacol. 2003;64(4):798-810.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C21H19N2O4F3S
Molecular Weight
452.44676
CAS #
353231-17-1
Related CAS #
LY487379 hydrochloride;353229-59-1
Appearance
Typically exists as solids (or liquids in special cases) at room temperature
SMILES
COC1=CC=CC=C1OC2=CC=C(C=C2)N(CC3=CN=CC=C3)S(=O)(=O)CC(F)(F)F
HS Tariff Code
2934.99.9001
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)
Solubility Data
Solubility (In Vitro)
DMSO : ~100 mg/mL (~221.02 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 10 mg/mL (22.10 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% 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 100.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.2102 mL 11.0509 mL 22.1019 mL
5 mM 0.4420 mL 2.2102 mL 4.4204 mL
10 mM 0.2210 mL 1.1051 mL 2.2102 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.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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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