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Methoxy-PEPy

CAT: 0804-HY-12510-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-12510-01Size:5 mg
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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].
CAS Number
524924-76-3
UNSPSC
12352005
Target
MGluR
Type
Reference compound
Related Pathways
GPCR/G Protein; Neuronal Signaling
Applications
Neuroscience-Neuromodulation
Field of Research
Neurological Disease
Assay Protocol
https://www.medchemexpress.com/Methoxy-PEPy.html
Purity
98.19
Solubility
DMSO : 100 mg/mL (ultrasonic)
Smiles
COC1=CC(C#CC2=NC=CC=C2)=CN=C1
Molecular Formula
C13H10N2O
Molecular Weight
210.23
References & Citations
[1]Cosford ND, et al. [3H]-methoxymethyl-MTEP and [3H]-methoxy-PEPy: potent and selective radioligands for the metabotropic glutamate subtype 5 (mGlu5) receptor. Bioorg Med Chem Lett. 2003 Feb 10;13 (3) :351-4.|[2]Anderson JJ, et al. In vivo receptor occupancy of mGlu5 receptor antagonists using the novel radioligand [3H]3-methoxy-5- (pyridin-2-ylethynyl) pyridine) . Eur J Pharmacol. 2003 Jul 18;473 (1) :35-40.|[3]Salisbury BG, et al. Inducible expression and pharmacological characterization of the mouse metabotropic glutamate 5b receptor. Eur J Pharmacol. 2008 Jan 28;579 (1-3) :34-9.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
MGluR5

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Alternative Products

CatalogName
BA5576-5.1Methoxy-PEPy
A21899-100Methoxy-PEPy 100mg
A21899-10Methoxy-PEPy 10mg
A21899-1Methoxy-PEPy 1mg
A21899-50Methoxy-PEPy 50mg
A21899-25Methoxy-PEPy 25mg
A21899-5Methoxy-PEPy 5mg
A21899-10mM-DMethoxy-PEPy 10mM * 1mL in DMSO
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