2. GPCR/G Protein Neuronal Signaling
  3. mGluR
  4. MTEP

MTEP 是一种有效的、非竞争性和高选择性的 mGluR5 拮抗剂。MTEP 表现出抗抑郁和抗焦虑的作用。MTEP 可以用于帕金森疾病的研究。

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MTEP Chemical Structure

MTEP Chemical Structure

CAS No. : 329205-68-7

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规格 是否有货
50 mg   询价  
100 mg   询价  
250 mg   询价  

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MTEP 的其他形式现货产品:

Customer Review

Other Forms of MTEP:

MTEP 相关抗体

Top Publications Citing Use of Products

查看 mGluR 亚型特异性产品:

查看所有亚型
mGluR1 mGluR2 mGluR3 mGluR4 mGluR5 mGluR6 mGluR7 mGluR8 mGluR

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MTEP is a potent, non-competitive and highly selective mGluR5 antagonist, with an IC50 of 5 nM and a Ki of 16 nM. MTEP shows antidepressant and anxiolytic-like effects. MTEP can be used for Parkinson's disease research[1][2][3][4]. MTEP is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

IC50 & Target

mGluR5

5 nM (IC50)

mGluR5

16 nM (Ki)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 IC50
12 nM
Compound: MTEP
Negative allosteric modulation of human mGluR5 expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay
Negative allosteric modulation of human mGluR5 expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay
[PMID: 23434029]
HEK293-A IC50
110 nM
Compound: 2, MTEP
Inverse agonist activity at rat mGluR5 expressed in HEK293A cells coexpressing Gqalpha assessed as inhibition of quisqualic-induced D-myo-inositol 1 production by ELISA
Inverse agonist activity at rat mGluR5 expressed in HEK293A cells coexpressing Gqalpha assessed as inhibition of quisqualic-induced D-myo-inositol 1 production by ELISA
[PMID: 22924094]
HEK293-A IC50
13.6 nM
Compound: 2
Antagonist activity at rat mGluR5 expressed in HEK293A cells assessed as glutamate-induced calcium flux preincubated for 140 sec before glutamate challenge by calcium fluorescence assay
Antagonist activity at rat mGluR5 expressed in HEK293A cells assessed as glutamate-induced calcium flux preincubated for 140 sec before glutamate challenge by calcium fluorescence assay
[PMID: 19445453]
体外研究
(In Vitro)

MTEP 对 mGluR5 的选择性高于 mGluR1，对其他 mGluR 亚型没有影响，并且比 MPEP (HY-14609A) 有更少的脱靶效应[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

MTEP 相关抗体:
体内研究
(In Vivo)

MTEP (0-5 mg/kg, 腹腔注射, 一次) 抑制由 Haloperidol (HY-14538) (0.5 mg/kg, 腹腔注射)诱导的僵直症[2]。
MTEP (0.3-3 mg/kg, 腹腔注射, 一次) 在雄性 C57BL/6J 小鼠中诱导抗抑郁样作用[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Wistar rats (215-315 g, 5-9/group)[2]
Dosage: 1, 3 and 5 mg/kg
Administration: IP, once, injected 60 min after Haloperidol (HY-14538) (0.5 mg/kg/2 ml i.p.)
Result: Inhibited the catalepsy induced by Haloperidol (HY-14538).
Animal Model: Male C57BL/6J mice (23-25 g)[3]
Dosage: 0.3, 1 and 3 mg/kg
Administration: IP, 1 h before the test
Result: Significantly decreased the immobility time of mice in the tail suspension test (TST) by 24%, 41% and 48%, respectively. The efficacy of MTEP used at doses of 1 and 3 mg/kg was not significantly different from that of Imipramine (HY-B1490A) (20 mg/kg, ip), used as a positive standard.
分子量

200.26

Formula

C11H8N2S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

MTEP 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:

MTEP329205-68-7mGluRMetabotropic glutamate receptorsAntidepressantanxiolytic-likeParkinson's diseaseInhibitorinhibitorinhibit

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产品名称：
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目录号：
HY-13206A
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