2. GPCR/G Protein Neuronal Signaling Protein Tyrosine Kinase/RTK JAK/STAT Signaling
  3. mGluR EGFR
  4. LY456236

LY456236 is a selective, non-competitive and orally active mGlu1 receptor antagonist that inhibits phosphoinositide hydrolysis with an IC50 of 0.145 μM. LY456236 also inhibits EGFR with an IC50 of 0.91 μM.

For research use only. We do not sell to patients.

LY456236 Chemical Structure

LY456236 Chemical Structure

CAS No. : 338736-46-2

Size Price Stock Quantity
5 mg USD 100 In-stock
10 mg USD 160 In-stock
25 mg USD 340 In-stock
50 mg USD 550 In-stock
100 mg   Get quote  
200 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

LY456236 Related Antibodies

Top Publications Citing Use of Products

View All mGluR Isoform Specific Products:

View All Isoforms
mGluR1 mGluR2 mGluR3 mGluR4 mGluR5 mGluR6 mGluR7 mGluR8 mGluR

View All EGFR Isoform Specific Products:

View All Isoforms
EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

LY456236 is a selective, non-competitive and orally active mGlu1 receptor antagonist that inhibits phosphoinositide hydrolysis with an IC50 of 0.145 μM. LY456236 also inhibits EGFR with an IC50 of 0.91 μM[1][3].

IC50 & Target

IC50: 0.145 μM (mGlu1), 0.91 μM (EGFR)[1]
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.

LY456236 Related Antibodies

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.
Molecular Weight

317.77

Formula

C16H16ClN3O2
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (786.73 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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1469 mL 15.7347 mL 31.4693 mL
5 mM 0.6294 mL 3.1469 mL 6.2939 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, 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
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, 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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.1469 mL 15.7347 mL 31.4693 mL 78.6733 mL
5 mM 0.6294 mL 3.1469 mL 6.2939 mL 15.7347 mL
10 mM 0.3147 mL 1.5735 mL 3.1469 mL 7.8673 mL
15 mM 0.2098 mL 1.0490 mL 2.0980 mL 5.2449 mL
20 mM 0.1573 mL 0.7867 mL 1.5735 mL 3.9337 mL
25 mM 0.1259 mL 0.6294 mL 1.2588 mL 3.1469 mL
30 mM 0.1049 mL 0.5245 mL 1.0490 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 1.5735 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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

LY456236 Related Classifications

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:

LY456236338736-46-2LY 456236LY-456236mGluREGFRMetabotropic glutamate receptorsEpidermal growth factor receptorErbB-1HER1anticonvulsantDHPGOCCM-30DBA/2CD1 miceseizureInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
LY456236
Cat. No.:
HY-103566
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

Request for HNMR Report

We have received your request and will respond to you as soon as possible.