Art. -Nr.: HY-103566

LY456236

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LY456236 is a selective, non-competitive and orally active antagonist of glutamate receptor 1 (mGlu1), which can inhibit phosphatidylinositol hydrolysis with an IC₅₀ of 0.145 μM. LY456236 can also inhibit EGFR, with an IC₅₀ of 0.918 μM. LY456236 blocks cell proliferation by inhibiting the MAPK pathway, reversing the anti-apoptotic effect of DHPG (HY-12598A). LY456236 can be used in epilepsy research.

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Reinheit: 99.57%
CAS. Nr.: 338736-46-2
Formel: C₁₆H₁₆ClN₃O₂
Molecular Weight:317.78

Speicherung:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

LY456236 Chemical Structure

CAS. Nr.: 338736-46-2

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Preis

Verfügbarkeit

Menge

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Top Publications Citing

Use of MCE Products

Antibody-Drug Conjugates

One-stop solution for XDC (ADC/PDC/RDC/ApDC/FDC/ISAC/VDC/SMDC)

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

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]^[2]

mGluR 1

EGFR

0.918 μM (IC₅₀)

Alle mGluR Isoform-spezifische Produkte anzeigen :

Alle EGFR Isoform-spezifische Produkte anzeigen :

Alle p38 MAPK Isoform-spezifische Produkte anzeigen :

In Vitro

LY456236 (2 μM; 30 min) reduces DHPG (HY-12598A)-stimulated OCCM-30 proliferation^[2].

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

Cell Proliferation Assay^[2]

Cell Line:

OCCM-30 cells
Concentration:

2 μM
Incubation Time:

30 min, followed by 72 h incubation with DHPG (HY-12598A)
Result:

Reduced DHPG-stimulated OCCM-30 proliferation.

In Vivo

LY456236 shows anticonvulsant effects in mice (3-100 mg/kg; i.p.; once) and rats (10-60 mg/kg; oral; once)^[3].

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

Animal Model:

DBA/2 mice and CD1 mice, seizure models^[3]
Dosage:

3-100 mg/kg
Administration:

IP, once
Result:

Produced dose-related anticonvulsant effects in preventing audiogenic-induced (tonic-clonic) seizures in DBA/2 mice, threshold electroshock-induced seizures in CD1 mice, and 6 Hz electroshock-induced seizures in CD1 mice.

Animal Model:

Amygdala-kindled Sprague-Dawley rats^[3]
Dosage:

10, 30 and 60 mg/kg
Administration:

Oral, once
Result:

Produced dose-related decreases in behavioral and electrographic seizures at threshold stimulus intensity. Produced a dose-related increase in the stimulus intensity required to produce generalized seizures.

Chemical Information

CAS. Nr. 338736-46-2
Appearance Solid
Molecular Weight 317.78
Formel C₁₆H₁₆ClN₃O₂
Color Light yellow to yellow
SMILES

COC1=CC=C(NC2=C3C=C(OC)C=CC3=NC=N2)C=C1.[H]Cl
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 250 mg/mL (786.71 mM; ultrasonic and warming and heat to 60°C; 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

3.1468 mL

15.7342 mL

31.4683 mL

5 mM

0.6294 mL

3.1468 mL

6.2937 mL

10 mM

0.3147 mL

1.5734 mL

3.1468 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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]. Ravikumar B, et al. Chemogenomic Analysis of the Druggable Kinome and Its Application to Repositioning and Lead Identification Studies. Cell Chem Biol. 2019 Nov 21;26(11):1608-1622.e6. [Content Brief]

[2]. Kanaya S, et al. Metabotropic glutamate receptor 1 promotes cementoblast proliferation via MAP kinase signaling pathways. Connect Tissue Res. 2016 Sep;57(5):417-26. [Content Brief]

[3]. Shannon HE, et al. Anticonvulsant effects of LY456236, a selective mGlu1 receptor antagonist. Neuropharmacology. 2005;49 Suppl 1:188-95. [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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.1468 mL	15.7342 mL	31.4683 mL	78.6708 mL
	5 mM	0.6294 mL	3.1468 mL	6.2937 mL	15.7342 mL
	10 mM	0.3147 mL	1.5734 mL	3.1468 mL	7.8671 mL
	15 mM	0.2098 mL	1.0489 mL	2.0979 mL	5.2447 mL
	20 mM	0.1573 mL	0.7867 mL	1.5734 mL	3.9335 mL
	25 mM	0.1259 mL	0.6294 mL	1.2587 mL	3.1468 mL
	30 mM	0.1049 mL	0.5245 mL	1.0489 mL	2.6224 mL
	40 mM	0.0787 mL	0.3934 mL	0.7867 mL	1.9668 mL
	50 mM	0.0629 mL	0.3147 mL	0.6294 mL	1.5734 mL
	60 mM	0.0524 mL	0.2622 mL	0.5245 mL	1.3112 mL
	80 mM	0.0393 mL	0.1967 mL	0.3934 mL	0.9834 mL
	100 mM	0.0315 mL	0.1573 mL	0.3147 mL	0.7867 mL

Keywords

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LY456236

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Kinase Inhibitor Library

MAPK Compound Library

Neuronal Signaling Compound Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Alle mGluR Isoform-spezifische Produkte anzeigen

Alle EGFR Isoform-spezifische Produkte anzeigen

Alle p38 MAPK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

LY456236 Related Classifications

HY-103566 Related Classifications