Art. -Nr.: HY-108707

LY3130481

1 Cited Publications

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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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Reinheit: 99.73%
CAS. Nr.: 1610802-47-5
Formel: C₁₉H₁₈N₄O₃S
Molecular Weight:382.44

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

LY3130481 Chemical Structure

CAS. Nr.: 1610802-47-5

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC50：65 nM (AMPA/TARP γ-8)^[1]

Alle iGluR Isoform-spezifische Produkte anzeigen :

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)	T_max (h)	C_max (ng/mL)	Cl_obs (mL•min/kg)	V_{dss_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.

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.

Chemical Information

CAS. Nr. 1610802-47-5
Appearance Solid
Molecular Weight 382.44
Formel C₁₉H₁₈N₄O₃S
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (1)

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Journal Impact Factor

Nat Commun

Modulatory mechanisms of TARP γ8-selective AMPA receptor therapeutics. [Abstract]

2023 Mar 25;14(1):1659. PMID: 36966141

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.6148 mL

13.0739 mL

26.1479 mL

5 mM

0.5230 mL

2.6148 mL

5.2296 mL

10 mM

0.2615 mL

1.3074 mL

2.6148 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Kelly L Knopp, et al. Modulation of TARP γ 8-Containing AMPA Receptors as a Novel Therapeutic Approach for Chronic Pain. J Pharmacol Exp Ther. 2019 Jun;369(3):345-363. [Content Brief]

[2]. Gardinier KM,et al. Discovery of the First α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptor Antagonist Dependent upon Transmembrane AMPA Receptor Regulatory Protein (TARP) γ-8. J Med Chem. 2016 May 26;59(10):4753-68. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

LY3130481

1 Cited Publications

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LY3130481

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Neuronal Signaling Compound Library

Orally Active Compound Library

Neurotransmitter Receptor Compound Library

Neuroprotective Compound Library

Anti-Parkinson's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Targeted Diversity Library

Antidepressant Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Ion Channel Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) LY3130481

Alle iGluR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

LY3130481

Membrane Transporter/Ion Channel Compound Library

Neuronal Signaling Compound Library

Orally Active Compound Library

Neurotransmitter Receptor Compound Library

Neuroprotective Compound Library

Anti-Parkinson's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Targeted Diversity Library

Antidepressant Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Ion Channel Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) LY3130481

Alle iGluR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

LY3130481 Related Classifications

HY-108707 Related Classifications