1. GPCR/G Protein
    Neuronal Signaling
  2. mGluR
  3. Methoxy-PEPy

Methoxy-PEPy 

Cat. No.: HY-12510 Purity: 98.19%
Handling Instructions

Methoxy-PEPy is a potent and highly selective mGlu5 receptor antagonist with IC50 of 1 nM.

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

Methoxy-PEPy Chemical Structure

Methoxy-PEPy Chemical Structure

CAS No. : 524924-76-3

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 99 In-stock
Estimated Time of Arrival: December 31
5 mg USD 90 In-stock
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10 mg USD 150 In-stock
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50 mg USD 450 In-stock
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100 mg USD 750 In-stock
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Description

Methoxy-PEPy is a potent and highly selective mGlu5 receptor antagonist with IC50 of 1 nM. IC50 value: 1 nM [1] Target: mGlu5R inhibitor Administration of [3H]methoxy-PEPy (50 microCi/kg i.v.) to mGlu5 receptor-deficient mice revealed binding at background levels in forebrain, whereas wild-type mice exhibited 14-fold higher binding in forebrain relative to cerebellum [2]. The calcium transients stimulated by these agonists were potently inhibited by reference allosteric mGlu5 antagonists - 2-methyl-6-(phenylethynyl)pyridine (MPEP), 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine (MTEP) and 3-methoxy-5-(pyridine-2-ylethynyl)pyridine (methoxy-PEPy) (IC(50) ranges: 0.8-66 nM) [3].

IC50 & Target[1]

mGlu5 Receptor

1 nM (IC50)

Molecular Weight

210.23

Formula

C₁₃H₁₀N₂O

CAS No.

524924-76-3

SMILES

COC1=CC(C#CC2=NC=CC=C2)=CN=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (475.67 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.7567 mL 23.7835 mL 47.5670 mL
5 mM 0.9513 mL 4.7567 mL 9.5134 mL
10 mM 0.4757 mL 2.3783 mL 4.7567 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 2.5 mg/mL (11.89 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (11.89 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (11.89 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 98.19%

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Keywords:

Methoxy-PEPymGluRMetabotropic glutamate receptorsInhibitorinhibitorinhibit

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Product Name:
Methoxy-PEPy
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HY-12510
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