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  1. GPCR/G Protein Neuronal Signaling
  2. mGluR
  3. MPEP Hydrochloride

MPEP Hydrochloride 是有效的、選擇性的、非競爭性的、口服有效的、具有系統(tǒng)活性的 mGlu5 受體拮抗劑,其完全抑制quisqualate 刺激的磷酸肌醇水解的 IC50 值為 36 nM。MPEP Hydrochloride 具有抗焦慮或抗抑郁活性。

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MPEP Hydrochloride Chemical Structure

MPEP Hydrochloride Chemical Structure

CAS No. : 219911-35-0

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in Water ¥330
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5 mg ¥300
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10 mg ¥500
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25 mg ¥950
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50 mg ¥1700
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100 mg ¥2700
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Customer Review

Other Forms of MPEP Hydrochloride:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻

生物活性

MPEP Hydrochloride is a potent, selective, noncompetitive, orally active and systemically active mGlu5 receptor antagonist, with an IC50 of 36 nM for completely inhibiting quisqualate-stimulated phosphoinositide (PI) hydrolysis. MPEP Hydrochloride has anxiolytic-or antidepressant-like effects[1][2]. MPEP (Hydrochloride) 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[1]

mGluR5

36 nM (IC50)

體外研究
(In Vitro)

MPEP does not show agonist or antagonist activity at 100 mM on human mGlu2, -3, -4a, -7b, and -8a receptors nor at 10 μM on the human mGlu6 receptor[1].

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

體內(nèi)研究
(In Vivo)

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[2].
MPEP (1-20 mg/kg) does shorten the immobility time in a tail suspension test in mice, however it is inactive in the behavioural despair test in rats[2].
MPEP (30 mg/kg i.p.) slightly but significantly increases (by 39%) the number of punished crossings in the four-plate test, lower doses of the compound (3 and 10 mg/kg) does not affect the number of punished crossings in that test (F (3,36)=3.240, P<0.05)[2].
MPEP (1, 10 and 20 mg/kg) significantly (by 55% after the highest dose), (F(3,28)=15.47, P<0.001) decreases the immobility time of mice in the tail suspension test. Its efficacy is similar to that of imipramine (20 mg/kg), used as the positive standard[2].

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

Animal Model: Male Wistar rats (200 ± 250 g)[2].
Dosage: IP or PO.
Administration: 0.3, 1 and 10 mg/kg, i.p. (Conflict drinking test).
Result: At a dose of 0.3 mg/kg was not ffective, at doses of 1 and 10 mg/kg i.p. significantly (F (3,30)=11.193, P<0.001), increased the number of shocks (by 330 and 507%, respectively) accepted during the experimental session in the Vogel test.
Animal Model: Male Wistar rats (200 ± 250 g)[2].
Dosage: IP or PO.
Administration: 1, 3 and 10 mg/kg, i.p. or 10 and 30 mg/kg, p.o.(Elevated plus-maze test).
Result: Administered at a dose of 1 mg kg71 i.p. did not change the entries into and time spent in the open arms. At doses of 3 and 10 mg/kg i.p. significantly (F (3,24)=22.978, P<0.001) dose-dependently increased the time spent in the open arms (up to 45 and 74%, respectively), and the percentage of entries into the open arms (up to 48 and 68%, respectively, F(3,24)=5.678, P<.01). At doses of 3 and 10 mg/kg i.p. significantly increased (by 64%) the total number of entries and reduced (by about 25%) the total time spent (data not shown) in the arms (either type).
At the dose of 30 mg/kg (po, but not 10 mg/kg) significantly (up to 64%, F (2,16)=14.249, P<0.001) increased the percentage of the time spent in the open arms and the percentage of entries into the open arms (up to 63%, F (2,16)=7.295, P<0.01). MPEP given p.o. in both doses used did not change the total number of entries nor the total time spent in the arms (either type).
分子量

229.70

Formula

C14H12ClN

CAS 號
性狀

固體

顏色

White to off-white

運輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性數(shù)據(jù)
細胞實驗: 

H2O 中的溶解度 : 25 mg/mL (108.84 mM; 超聲助溶 (<80°C))

配制儲備液
濃度 溶劑體積 質量 1 mg 5 mg 10 mg
1 mM 4.3535 mL 21.7675 mL 43.5350 mL
5 mM 0.8707 mL 4.3535 mL 8.7070 mL
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復凍融造成的產(chǎn)品失效
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲存時,請在6個月內(nèi)使用,-20°C儲存時,請在1個月內(nèi)使用。

* 備注:如您選擇水作為儲備液,請稀釋至工作液后,再用 0.22 μm 的濾膜過濾除菌后使用。

  • 摩爾計算器

  • 稀釋計算器

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

質量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物實驗:

以下溶解方案,請直接配制工作液。建議現(xiàn)用現(xiàn)配,在短期內(nèi)盡快用完。 以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比; 如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶。

  • 方案 一

    請依序添加每種溶劑: Saline

    Solubility: 100 mg/mL (435.35 mM); 澄清溶液; 超聲助溶

動物溶解方案計算器
請輸入動物實驗的基本信息:

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

由于實驗過程有損耗,建議您多配一只動物的量
計算結果
工作液所需濃度 : mg/mL
該產(chǎn)品水溶性佳,請具體參考實測 水 / PBS / Saline 中的溶解度數(shù)據(jù)。
您所需的儲備液濃度超過該產(chǎn)品的實測溶解度,如有需要,請與 MCE 中國技術支持聯(lián)系。
純度 & 產(chǎn)品資料

純度: 99.82%

參考文獻

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲存時,請在6個月內(nèi)使用,-20°C儲存時,請在1個月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質量 1 mg 5 mg 10 mg 25 mg
H2O 1 mM 4.3535 mL 21.7675 mL 43.5350 mL 108.8376 mL
5 mM 0.8707 mL 4.3535 mL 8.7070 mL 21.7675 mL
10 mM 0.4354 mL 2.1768 mL 4.3535 mL 10.8838 mL
15 mM 0.2902 mL 1.4512 mL 2.9023 mL 7.2558 mL
20 mM 0.2177 mL 1.0884 mL 2.1768 mL 5.4419 mL
25 mM 0.1741 mL 0.8707 mL 1.7414 mL 4.3535 mL
30 mM 0.1451 mL 0.7256 mL 1.4512 mL 3.6279 mL
40 mM 0.1088 mL 0.5442 mL 1.0884 mL 2.7209 mL
50 mM 0.0871 mL 0.4354 mL 0.8707 mL 2.1768 mL
60 mM 0.0726 mL 0.3628 mL 0.7256 mL 1.8140 mL
80 mM 0.0544 mL 0.2721 mL 0.5442 mL 1.3605 mL
100 mM 0.0435 mL 0.2177 mL 0.4354 mL 1.0884 mL

* 備注:如您選擇水作為儲備液,請稀釋至工作液后,再用 0.22 μm 的濾膜過濾除菌后使用。

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.

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產(chǎn)品名稱:
MPEP Hydrochloride
目錄號:
HY-14609
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