2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. iGluR
  4. LY3130481

LY3130481 is an orally available AMPA receptor antagonist, selectively inhibiting the IC50 value of AMPA/TARP γ-8 at 65 nM. LY3130481 has anticonvulsant, antiepileptic, and pain-relieving effects.

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LY3130481 Chemical Structure

LY3130481 Chemical Structure

CAS No. : 1610802-47-5

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

LY3130481 Related Antibodies

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1 Publications Citing Use of MCE LY3130481

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AMPA Receptor NMDA Receptor Kainate Receptor

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Description

LY3130481 is an orally available AMPA receptor antagonist, selectively inhibiting the IC50 value of AMPA/TARP γ-8 at 65 nM. LY3130481 has anticonvulsant, antiepileptic, and pain-relieving effects[1][2].

IC50 & Target

IC50：65 nM (AMPA/TARP γ-8)[1]
In Vitro

LY3130481 can effectively inhibit AMPA receptor-mediated currents in hippocampal and cortical neurons, but it has a weaker effect in cerebellar Purkinje cells. Similar effects were not observed in neurons from γ8 gene knockout mice[1].
Pharmacokinetic Analysis in Rats[2]

Route Dose (mg/kg) AUC (ng•h/mL) Tmax (h) Cmax (ng/mL) Clobs (mL•min/kg) Vdss_obs (mL/kg) F (%)
i.v. 1 1470 / / 11.4 1280 /
p.o. 3 4220 1.3 628 / / 97

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

LY3130481 Related Antibodies
In Vivo

LY3130481 (1-30 mg/kg, oral, single dose) reduces the pain response in rats induced by formaldehyde, with an ED50 value of about 3.7 mg/kg[1].
LY3130481 (0.3-30 mg/kg, i.v., single dose) decreases the wind-up discharge of C-fiber inputs to WDR (wide dynamic range) neurons in a dose-dependent manner[1].
LY3130481 (1 mg/kg, i.v.; 3 mg/kg, p.o.; single dose) has low clearance rates in rats and good bioavailability[2].
LY3130481 (1-100 mg/kg, oral or p.o., single dose) shows anticonvulsant effects in rats, with an ED50 of 1.7 mg/kg, providing anticonvulsant effects at ten times the high dose without motor impairment[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Rats induced by the drug pentatetrazole (PTZ)[2]
Dosage: 1, 3, 10, 30 mg/kg; 10, 100 mg/kg; single dose
Administration: Oral
Result: Protected against clonic seizures, with an ED50 of 1.7 mg/kg, and did not significantly impair the ability of rats to climb to the top of the screen when inverted at a dose of 30 mg/kg. At a dose of 30 mg/kg, behavior was completely impaired, with a TD50of 3.8 mg/kg.
Animal Model: Male Sprague Dawley (SD) rats [2]
Dosage: 0.3-30 mg/kg; 1, 3, 10 and 30 mg/kg
Administration: Intravenous injection (i.v.); Oral
Result: Reduced C fiber input to WDR (wide dynamic range) neurons' wind-up discharge in intravenous injection experiments.Decreased formalin-induced pain behavior in rats, with an ED50 value of approximately 3.7 mg/kg when administered orally.
Molecular Weight

382.44

Formula

C19H18N4O3S
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(N1)SC2=C1C=CC([C@H](C)C3=NN(C4=CC=C(OCCO)C=N4)C=C3)=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (653.70 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6148 mL 13.0739 mL 26.1479 mL
5 mM 0.5230 mL 2.6148 mL 5.2296 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (5.44 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (5.44 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
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%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6148 mL 13.0739 mL 26.1479 mL 65.3697 mL
5 mM 0.5230 mL 2.6148 mL 5.2296 mL 13.0739 mL
10 mM 0.2615 mL 1.3074 mL 2.6148 mL 6.5370 mL
15 mM 0.1743 mL 0.8716 mL 1.7432 mL 4.3580 mL
20 mM 0.1307 mL 0.6537 mL 1.3074 mL 3.2685 mL
25 mM 0.1046 mL 0.5230 mL 1.0459 mL 2.6148 mL
30 mM 0.0872 mL 0.4358 mL 0.8716 mL 2.1790 mL
40 mM 0.0654 mL 0.3268 mL 0.6537 mL 1.6342 mL
50 mM 0.0523 mL 0.2615 mL 0.5230 mL 1.3074 mL
60 mM 0.0436 mL 0.2179 mL 0.4358 mL 1.0895 mL
80 mM 0.0327 mL 0.1634 mL 0.3268 mL 0.8171 mL
100 mM 0.0261 mL 0.1307 mL 0.2615 mL 0.6537 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

LY31304811610802-47-5LY 3130481LY-3130481iGluRIonotropic glutamate receptorsProtection against convulsionAnti-epilepsyAnalgesiaInhibitorinhibitorinhibit

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