| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
LY487379 targets the metabotropic glutamate receptor subtype 2 (mGluR2), a G protein-coupled receptor that modulates neurotransmitter release in the central nervous system. As a positive allosteric modulator, LY487379 binds to a site on the receptor that is distinct from the orthosteric (glutamate) binding site and enhances the receptor's response to glutamate. This allosteric modulation increases the efficacy of glutamate without directly activating the receptor. The compound exhibits an EC50 of 1.7 μM for mGlu2 and shows selectivity over mGlu3 (EC50 > 10 μM).
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| ln Vitro |
In vitro, LY487379 functions as a selective positive allosteric modulator of mGluR2. It enhances glutamate-stimulated [35S]GTPγS binding to mGlu2 receptors with an EC50 of 1.7 μM. The compound shows no intrinsic agonist or antagonist activity at mGluR2 and has no activity at mGlu3 receptors. These in vitro studies confirm the compound's mechanism of action as a selective PAM of mGluR2.
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| ln Vivo |
LY487379 hydrochloride (intraperitoneal injection; 30 mg/kg; injected 30 min before the test) significantly reduces the number of trials needed to meet the criteria in the attentional set-shifting task during the ED phase of the ASST in male Sprague-Dawley rats. However, during any other stage of discrimination, there is no discernible drug effect[1].
LY487379 hydrochloride (intraperitoneal injection; 10-30 mg/kg) causes the microdialysate norepinephrine levels to rise; the dose-effect relationship increased in the form of a bell. Additionally, in male Sprague-Dawley rats, it dose-dependently raises the levels of extracellular serotonin in the medial prefrontal cortex[1]. In vivo, LY487379 has been studied for its effects on cognitive flexibility and body temperature. The compound promotes cognitive flexibility, suggesting potential benefits in psychiatric disorders such as schizophrenia. It also exhibits anti-hyperthermic effects, indicating potential applications in conditions involving elevated body temperature. Further in vivo studies would be required to fully characterize its therapeutic potential. |
| Enzyme Assay |
The in vitro enzyme/receptor binding (non-cellular) assays for LY487379 are radioligand binding assays using membrane preparations from cells expressing recombinant human mGluR2 or mGluR3 receptors. The compound's ability to enhance glutamate-stimulated [35S]GTPγS binding is measured to assess its PAM activity. The EC50 for enhancement of [35S]GTPγS binding is determined from dose-response curves. These assays confirm the compound's selective PAM activity at mGluR2.
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| Cell Assay |
In vitro cellular assays for LY487379 are performed using cell lines expressing recombinant mGluR2 receptors. Cells are treated with LY487379 in the presence of a submaximal concentration of glutamate, and receptor activation is assessed by measuring downstream signaling events such as inhibition of cAMP accumulation or calcium mobilization. The compound's ability to enhance glutamate-stimulated signaling is measured. These assays confirm the functional PAM activity of LY487379 at mGluR2.
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| Animal Protocol |
In vivo animal experiments for LY487379 are conducted in rodent models to study cognitive function and thermoregulation. Mice or rats are administered LY487379 via oral or intraperitoneal injection, and cognitive performance is assessed using behavioral tests such as the Morris water maze or novel object recognition. Body temperature is monitored to evaluate the compound's anti-hyperthermic effects. These studies provide evidence for the compound's in vivo activity and potential therapeutic applications.
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| ADME/Pharmacokinetics |
LY487379 HCl has a molecular weight of 488.91 g/mol and a molecular formula of C21H19F3N2O4S•HCl. The compound is soluble in DMSO at concentrations ≥20 mg/mL. Detailed pharmacokinetic parameters such as bioavailability, half-life, and tissue distribution have not been extensively reported in the available literature. However, the compound's in vivo efficacy in animal models suggests adequate systemic exposure following oral administration.
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| Toxicity/Toxicokinetics |
LY487379 HCl has been evaluated in preclinical studies and has been reported to be well-tolerated at effective doses. No significant toxicity has been reported in the available literature. However, comprehensive toxicology studies would be necessary to fully assess the compound's safety profile for clinical development. As a selective mGluR2 PAM, LY487379 may have a favorable safety profile with reduced risk of off-target effects.
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| References |
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| Additional Infomation |
LY487379 HCl is a selective positive allosteric modulator of mGluR2 with an EC50 of 1.7 μM for enhancing glutamate-stimulated [35S]GTPγS binding. It shows no activity at mGlu3 receptors and no intrinsic agonist or antagonist activity at mGluR2. The compound promotes cognitive flexibility and has anti-hyperthermic effects. LY487379 is a research compound with potential applications in psychiatric and neurological disorders. It is not an approved drug.
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| Molecular Formula |
C21H20CLF3N2O4S
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| Molecular Weight |
488.9077
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| Exact Mass |
488.078
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| Elemental Analysis |
C, 51.59; H, 4.12; Cl, 7.25; F, 11.66; N, 5.73; O, 13.09; S, 6.56
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| CAS # |
353229-59-1
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| Related CAS # |
LY487379; 353231-17-1
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| PubChem CID |
56972206
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| Appearance |
Solid powder
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| LogP |
6.664
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
32
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| Complexity |
648
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| Defined Atom Stereocenter Count |
0
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| SMILES |
COC1=CC=CC=C1OC2=CC=C(C=C2)N(CC3=CN=CC=C3)S(=O)(=O)CC(F)(F)F.Cl
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| InChi Key |
LPWFRDWTOKLHJC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H19F3N2O4S.ClH/c1-29-19-6-2-3-7-20(19)30-18-10-8-17(9-11-18)26(14-16-5-4-12-25-13-16)31(27,28)15-21(22,23)24;/h2-13H,14-15H2,1H3;1H
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| Chemical Name |
2,2,2-trifluoro-N-[4-(2-methoxyphenoxy)phenyl]-N-(pyridin-3-ylmethyl)ethanesulfonamide;hydrochloride
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| Synonyms |
LY 487379; LY-487,379; LY 487,379; LY487,379; LY487379 HCl; LY-487379
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0454 mL | 10.2268 mL | 20.4537 mL | |
| 5 mM | 0.4091 mL | 2.0454 mL | 4.0907 mL | |
| 10 mM | 0.2045 mL | 1.0227 mL | 2.0454 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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