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WAY-303290

Cat No.:V41861 Purity: ≥98%
GluR6 antagonist-1 is a benzothiophene analogue that works as a GluR6 antagonist.
WAY-303290
WAY-303290 Chemical Structure CAS No.: 323176-64-3
Product category: iGluR
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
25mg
50mg
100mg
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Product Description
GluR6 antagonist-1 is a benzothiophene analogue that works as a GluR6 antagonist. GluR6 antagonist-1 may be utilized to study acute and chronic neurological diseases
WAY-303290 (GluR6 antagonist-1) is a benzothiophene derivative acting as an ionotropic glutamate receptor 6 (GluR6) antagonist. It can be used for researching acute and chronic neurological disorders. The compound's molecular formula is C15H11ClN2OS with a molecular weight of 302.78. WAY-303290 is a research tool for studying glutamatergic signaling and its role in neurological diseases.
Biological Activity I Assay Protocols (From Reference)
Targets
WAY-303290 targets GluR6 (also known as GRIK2), an ionotropic glutamate receptor belonging to the kainate receptor family. GluR6 is a ligand-gated ion channel that mediates fast excitatory neurotransmission in the central nervous system and is involved in synaptic plasticity, learning, and memory. By acting as a GluR6 antagonist, WAY-303290 blocks glutamate-induced ion flux through the receptor, thereby modulating glutamatergic signaling.
ln Vitro
In vitro, WAY-303290 is a benzothiophene derivative that acts as an ionotropic glutamate receptor 6 (GluR6) antagonist. It inhibits the pY binding site of the tyrosine kinase p56lck SH2 domain. The compound's antagonism of GluR6 makes it valuable for studying the role of kainate receptors in neurological disorders. However, specific IC50 values and detailed in vitro activity data have not been reported in the available literature.
ln Vivo
In vivo, WAY-303290 has potential applications in researching acute and chronic neurological disorders. By antagonizing GluR6, the compound may modulate glutamatergic signaling and have therapeutic potential for conditions involving glutamate excitotoxicity. However, specific in vivo efficacy data for WAY-303290 have not been detailed in the available literature. Further preclinical studies would be required.
Enzyme Assay
For in vitro receptor binding and functional assays, cells expressing GluR6 receptors are incubated with radiolabeled ligands or agonists at various concentrations of WAY-303290 (0.1-100 µM). Receptor binding affinity is measured using radioligand binding assays. Functional antagonism is assessed by measuring calcium flux or electrophysiological recordings in response to glutamate stimulation in the presence of the compound.
Cell Assay
For cell-based assays, neurons or cell lines expressing GluR6 are treated with WAY-303290 at concentrations ranging from 0.1-100 µM. Receptor activation is assessed by measuring calcium influx using calcium-sensitive fluorescent dyes or by electrophysiological recordings. Cell viability and neurotoxicity can also be assessed in models of glutamate excitotoxicity.
Animal Protocol
For in vivo studies, animal models of neurological disorders such as epilepsy, stroke, or neurodegenerative diseases would be used. WAY-303290 would be administered via appropriate routes at doses determined from pharmacokinetic studies. Neurological outcomes, seizure activity, or neuroprotection would be assessed. However, specific in vivo protocols for WAY-303290 have not been detailed in the available literature.
ADME/Pharmacokinetics
WAY-303290 is soluble in DMSO. Storage is recommended at -20°C for 3 years (powder) or -20°C for 1 month or -80°C for 6 months in solvent. Further detailed PK parameters including half-life, oral bioavailability, and tissue distribution would be required for in vivo studies. The compound is for research use only and is not intended for human or veterinary use.
Toxicity/Toxicokinetics
Toxicological data for WAY-303290 have not been extensively reported. As a research compound, it is intended for laboratory use only and is not for human or veterinary use. Standard safety precautions should be followed when handling this compound. Comprehensive toxicology studies would be required before any clinical development.
References
:Immunomodulatory compounds that target and inhibit the py'binding site of tyrosene kinase p56 lck sh2 domain. US20070099970A1.
Additional Infomation
WAY-303290 (GluR6 antagonist-1) is a benzothiophene derivative acting as an ionotropic glutamate receptor 6 (GluR6) antagonist. It can be used for researching acute and chronic neurological disorders. WAY-303290 is a research tool for studying glutamatergic signaling and neurological diseases. It is not approved for clinical use.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C15H11CLN2OS
Molecular Weight
302.78
Exact Mass
302.028
CAS #
323176-64-3
PubChem CID
673385
Appearance
Yellow to brown solid powder
Density
1.4±0.1 g/cm3
Boiling Point
543.5±50.0 °C at 760 mmHg
Flash Point
282.5±30.1 °C
Vapour Pressure
0.0±1.5 mmHg at 25°C
Index of Refraction
1.688
LogP
3.71
Hydrogen Bond Donor Count
1
Hydrogen Bond Acceptor Count
3
Rotatable Bond Count
3
Heavy Atom Count
20
Complexity
355
Defined Atom Stereocenter Count
0
SMILES
C1=CC=C2C(=C1)C(=C(S2)C(=O)NCC3=CN=CC=C3)Cl
InChi Key
FLKPRONUHHJNKH-UHFFFAOYSA-N
InChi Code
InChI=1S/C15H11ClN2OS/c16-13-11-5-1-2-6-12(11)20-14(13)15(19)18-9-10-4-3-7-17-8-10/h1-8H,9H2,(H,18,19)
Chemical Name
3-chloro-N-(pyridin-3-ylmethyl)-1-benzothiophene-2-carboxamide
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)
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
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
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution 50 μL Tween 80 850 μL Saline)
*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 : PEG300Tween 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).
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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)]
*Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO 100 μLPEG300 200 μL castor oil 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH 400 μLPEG300 50 μL Tween 80 450 μL 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).
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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders


Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.3027 mL 16.5136 mL 33.0273 mL
5 mM 0.6605 mL 3.3027 mL 6.6055 mL
10 mM 0.3303 mL 1.6514 mL 3.3027 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.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

  • Calculate the Mass of a compound required to prepare a solution of known volume and concentration
  • Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume
An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
  • To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
  • Click the “Calculate” button
  • The answer appears in the Volume (to add to vial) box
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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