MPEP - Moligand™, 10mM in DMSO , Allosteric modulator of mGlu 4 receptor;Allosteric modulator of mGlu 5 receptor, CAS No.96206-92-7, Allosteric modulator of mGlu 4 receptor;Allosteric modulator of mGlu 5 receptor

CAS: 96206-92-7 Cat. No.: M408882 分子式: C₁₄H₁₁N 分子量: 193.24

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

2-methyl-6-(2-phenylethynyl)pyridine

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

概要

Information

MPEP is a selectivemGlu5receptor antagonist withIC50of 36 nM, exhibits no appreciable activity at mGlu1b/2/3/4a/7b/8a/6 receptors.
In vitro

MPEP has no appreciable agonist or antagonist activity at the closely related recombinant human mGlu1b receptor expressed in CHO-K1 cells or a purinoreceptor endogenously expressed in L(tk^-) cells up to concentrations of 100 μM. Furthermore, MPEP shows no appreciable agonist or antagonist activity in cAMP accumulation or [³⁵S]-GTPγS binding assays at the recombinant human group II and III metabotropic receptors (human mGlu2, -3, -4a, -6, -7b, -8a) as well as the human NMDA (NMDAR1A/2A, -1A/2B), rat AMPA (GluR3) and human kainate (GluR6) receptor subtypes. In slices of rat neonatal hippocampus, striatum, and cortex but not cerebellum, MPEP inhibits DHPG-stimulated PI hydrolysis with IC50 of 8.0 nM, 20.5 nM, and 17.9 nM, respectively. MPEP positively modulates the hmGluR4 in a recombinant expression system, and the effect of MPEP is fully dependent on the activation of the orthosteric agonist _L-AP4.

In vivo

When microiontophoretically applied into the brain of rats, MPEP reduces DHPG-induced excitations but not the excitations induced by AMPA. Following intravenous administration, MPEP produces a dose-dependent inhibition of DHPG-induced but not AMPA-induced excitations with a rapid onset of action. Oral administration of MPEP also exhibits excellent anti-hyperalgesic activity in the Complete Freund\'s Adjuvant and turpentine models of inflammatory pain. MPEP (1-30 mg/kg) induces anxiolytic-like effects in the conflict drinking test and the elevated plus-maze test in rats as well as in the four-plate test in mice. MPEP (1-20 mg/kg) shortens the immobility time in a tail suspension test in mice, but it is inactive in the behavioural despair test in rats. MPEP has no effect on locomotor activity or motor coordination. MPEP significantly reduces fmr1 but not wild-type center square entries and duration. In open field tests, MPEP reduces fmr1^tm1Cgr center field behavior to one indistinguishable from wild-type. MPEP produces a significant reduction of total locomotor activity in three of four groups tested, at both 10 mg/kg and 30 mg/kg.
Cell Data

cell lines：SKOV-3 cells

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

同義語

2-methyl-6-(2-phenylethynyl)pyridine

仕様と純度

Moligand™, 10mM in DMSO

生化学的・生理学的メカニズム

MPEP is a selective mGlu5 receptor antagonist with IC50 of 36 nM, exhibits no appreciable activity at mGlu1b/2/3/4a/7b/8a/6 receptors.

保管条件

Store at -80°C

入荷

Dry ice packs + Cold packs

この製品は冷冷この冷このこの製品の運送が必要です。地上およびその他の経済サービスは利用できません。

等級

Moligand™

アクションタイプ

ALLOSTERIC MODULATOR

作用メカニズム

Allosteric modulator of mGlu 4 receptor;Allosteric modulator of mGlu 5 receptor

名前と識別子

• 異性体SMILES: CC1=NC(=CC=C1)C#CC2=CC=CC=C2
• 分子量: 193.24
• Reaxy-Rn: 140513
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=140513&ln=

関連ターゲット（人間）

CYP1A2 Tchem Cytochrome P450 1A2 (1 Activities)

Discover Target: CYP1A2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

GRM1 Tchem Metabotropic glutamate receptor 1 (1 Activities)

Discover Target: GRM1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

GRM5 Tchem Metabotropic glutamate receptor 5 (29 Activities)

Discover Target: GRM5

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

化学的性質と物理的性質

• 溶解度: Solubility (25°C) In vitro Ethanol: 58 mg/mL (199.69 mM); DMSO: 29 mg/mL warmed with 50ºC Water: bath (99.84 mM); Water: Insoluble
• 融点（°C）: 47 °C

よくある質問

What is Moligand??

Moligand? is one of Aladdin Scientific's premium product lines, formulated for high-purity applications across multiple workflows. Compared to standard grades in the same workflow, Moligand? products typically offer tighter specifications, more rigorous QC, and stronger lot-to-lot consistency.

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 96206-92-7, the molecular formula is C14H11N, and the molecular weight is 193.24 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.