| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| M408882-1ml |
1ml |
现货  |
|
| 英文别名 | 2-methyl-6-(2-phenylethynyl)pyridine |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | MPEP |
| 生化机理 | MPEP 是一种选择性 mGlu5 受体拮抗剂，IC50 为 36 nM，对 mGlu1b/2/3/4a/7b/8a/6 受体无明显活性。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 变构调节剂 |
| 作用机制 | mGlu 4 受体的异位调节剂;mGlu 5 受体的异位调节剂 |
| 产品介绍 |
MPEP是mGlu5受体非竞争性拮抗剂，IC50为36 nM，还是mGlu4受体的正向变构调节剂。 Information MPEP is a selectivemGlu5receptor antagonist withIC50of 36 nM, exhibits no appreciable activity at mGlu1b/2/3/4a/7b/8a/6 receptors. 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 fmr1tm1Cgr 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 lines：SKOV-3 cells Concentrations： Incubation Time： Powder Purity:≥99% |
| IC50 | mGluR5, IC50: 36 nM |
|---|---|
| ALogP | 3.499 |
| hba_count | 1 |
| Rotatable Bond | 2 |
| 分子类型 | 小分子 |
|---|---|
| Canonical 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= |
| 溶解性 | 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; |
|---|---|
| DMSO(mg / mL) Max Solubility | 39 |
| DMSO(mM) Max Solubility | 201.82 |
| Water(mg / mL) Max Solubility | <1 |
| Reaxy-Rn | 140513 |
|---|---|
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=140513&ln= |
| Record the entire process by video | Conform |
|---|---|
| Concentration(Compounding value) | 9-11（mmol/L） |
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