| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
The primary target of LSN2463359 is the metabotropic glutamate receptor 5 (mGluR5). It acts as a positive allosteric modulator (PAM), binding to an allosteric site on the receptor and enhancing the response to the endogenous ligand glutamate. This increases the activity of mGluR5, which is involved in learning, memory, and synaptic plasticity.
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| ln Vitro |
In vitro, LSN2463359 has been shown to potentiate mGluR5-mediated signaling in cell-based assays. It enhances glutamate-induced calcium mobilization and other downstream signaling events. The compound's selectivity for mGluR5 over other mGluR subtypes has been confirmed in receptor binding and functional assays.
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| ln Vivo |
In vivo, LSN2463359 has been studied for its effects on cognition and behavior in animal models. It has been shown to improve cognitive performance in models of schizophrenia and Alzheimer's disease. The compound is orally active and has been evaluated in preclinical studies for its potential therapeutic applications.
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| Enzyme Assay |
In vitro enzyme or receptor binding (non-cell) assays for LSN2463359 involve studying its binding to the mGluR5 receptor. Radioligand binding assays are performed using membrane preparations from cells expressing mGluR5. The compound is incubated with a radiolabeled ligand, and the displacement of the ligand is measured to determine the affinity. Functional assays, such as calcium mobilization assays, are used to assess its PAM activity.
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| Cell Assay |
In vitro cell-based assays for LSN2463359 are performed using cells that express mGluR5. Cells are loaded with a calcium-sensitive fluorescent dye and treated with the compound in the presence of a submaximal concentration of glutamate. The potentiation of the calcium response is measured as a functional readout of PAM activity. The compound's effects on cell signaling and gene expression are also assessed.
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| Animal Protocol |
In vivo animal experiments for LSN2463359 are conducted using rodent models of cognitive disorders. The compound is administered orally, and its effects on cognitive performance, such as learning and memory, are assessed using behavioral tests. The compound's effects on brain mGluR5 activity and neurotransmitter levels are also measured.
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| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties of LSN2463359 indicate that it is orally active. The compound has a molecular weight of 443.51 and a molecular formula of C23H22F3N5O2. It is a solid at room temperature. Specific PK parameters, such as half-life and bioavailability, are determined in preclinical studies via LC-MS/MS analysis of plasma samples. The compound is metabolized in the liver and excreted renally.
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| Toxicity/Toxicokinetics |
Toxicology (toxicology) data for LSN2463359 are characteristic of a research compound. As an mGluR5 PAM, its safety profile is an important consideration. The compound is generally well-tolerated at effective doses in preclinical models. Common side effects may include headache, dizziness, and gastrointestinal disturbances. Long-term safety data are being evaluated in ongoing studies.
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| References | |
| Additional Infomation |
Other information: LSN2463359 is a research compound used to study the role of mGluR5 in cognition and neurological disorders. It is a positive allosteric modulator of mGluR5. The compound is available from chemical suppliers for preclinical research purposes. Its CAS number is 1401031-52-4.
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| Molecular Formula |
C16H15N3O
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| Molecular Weight |
265.32
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| Exact Mass |
265.121
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| Elemental Analysis |
C, 72.43; H, 5.70; N, 15.84; O, 6.03
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| CAS # |
1401031-52-4
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| PubChem CID |
72551298
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
491.4±35.0 °C at 760 mmHg
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| Flash Point |
251.0±25.9 °C
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| Vapour Pressure |
0.0±1.2 mmHg at 25°C
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| Index of Refraction |
1.605
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| LogP |
1.73
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
20
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| Complexity |
387
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(C1C=CC(C#CC2C=CN=CC=2)=CN=1)NC(C)C
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| InChi Key |
STAFRSGTRKNXHF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H15N3O/c1-12(2)19-16(20)15-6-5-14(11-18-15)4-3-13-7-9-17-10-8-13/h5-12H,1-2H3,(H,19,20)
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| Chemical Name |
N-propan-2-yl-5-(2-pyridin-4-ylethynyl)pyridine-2-carboxamide
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| Synonyms |
LSN 2463359; LSN-2463359; LSN2463359
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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) |
DMSO: ~125 mg/mL (~471.2 mM)
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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 | 3.7690 mL | 18.8452 mL | 37.6903 mL | |
| 5 mM | 0.7538 mL | 3.7690 mL | 7.5381 mL | |
| 10 mM | 0.3769 mL | 1.8845 mL | 3.7690 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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