2. GPCR/G Protein Neuronal Signaling
  3. mGluR
  4. VU0360172

VU0360172 is a potent and selective mGlu5 receptor positive allosteric modulator with an EC50 value of 16 nM and a Ki of 195 nM, respectively. VU0360172 stimulates polyphosphoinositide (PI) hydrolysis in vivo, which is abrogated in mGlu5 receptors gene deleted mice. VU0360172 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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VU0360172

VU0360172 構造式

CAS 番号 : 1310012-12-4

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 165 在庫あり
Solution
10 mM * 1 mL in DMSO USD 165 在庫あり
Solid
5 mg $150 在庫あり
10 mg $240 在庫あり
25 mg $480 在庫あり
50 mg $750 在庫あり
100 mg   お問い合わせ  
200 mg   お問い合わせ  

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Based on 0 publication(s) in Google Scholar

Other Forms of VU0360172:

VU0360172 関連抗体

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mGluR アイソフォーム固有の製品をすべて表示:

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mGluR1 mGluR2 mGluR3 mGluR4 mGluR5 mGluR6 mGluR7 mGluR8 mGluR

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製品説明

VU0360172 is a potent and selective mGlu5 receptor positive allosteric modulator with an EC50 value of 16 nM and a Ki of 195 nM, respectively. VU0360172 stimulates polyphosphoinositide (PI) hydrolysis in vivo, which is abrogated in mGlu5 receptors gene deleted mice[1]. VU0360172 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

16 nM (EC50)

mGluR5

195 nM (Ki)

Cellular Effect
Cell Line Type Value Description References
CHO EC50
39 nM
Compound: 26, VU0360172
Positive allosteric modulation of rat mGluR5 stably expressed in CHO cells assessed as calcium mobilization
Positive allosteric modulation of rat mGluR5 stably expressed in CHO cells assessed as calcium mobilization
[PMID: 24050755]
HEK293 EC50
16 nM
Compound: 3, VU0360172
Positive allosteric modulation of rat mGluR5 expressed in human HEK293 cells assessed as calcium mobilization
Positive allosteric modulation of rat mGluR5 expressed in human HEK293 cells assessed as calcium mobilization
[PMID: 22981332]
分子量

294.32

分子式

C18H15FN2O
CAS 番号
Appearance

Solid

Color

Light yellow to brown

SMILES

O=C(NC1CCC1)C2=CC=C(N=C2)C#CC3=CC=CC(F)=C3
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶剤 & 溶解度
体外: 

DMSO : 83.33 mg/mL (283.13 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.3977 mL 16.9883 mL 33.9766 mL
5 mM 0.6795 mL 3.3977 mL 6.7953 mL
10 mM 0.3398 mL 1.6988 mL 3.3977 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: 2.08 mg/mL (7.07 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.08 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.3977 mL 16.9883 mL 33.9766 mL 84.9416 mL
5 mM 0.6795 mL 3.3977 mL 6.7953 mL 16.9883 mL
10 mM 0.3398 mL 1.6988 mL 3.3977 mL 8.4942 mL
15 mM 0.2265 mL 1.1326 mL 2.2651 mL 5.6628 mL
20 mM 0.1699 mL 0.8494 mL 1.6988 mL 4.2471 mL
25 mM 0.1359 mL 0.6795 mL 1.3591 mL 3.3977 mL
30 mM 0.1133 mL 0.5663 mL 1.1326 mL 2.8314 mL
40 mM 0.0849 mL 0.4247 mL 0.8494 mL 2.1235 mL
50 mM 0.0680 mL 0.3398 mL 0.6795 mL 1.6988 mL
60 mM 0.0566 mL 0.2831 mL 0.5663 mL 1.4157 mL
80 mM 0.0425 mL 0.2124 mL 0.4247 mL 1.0618 mL
100 mM 0.0340 mL 0.1699 mL 0.3398 mL 0.8494 mL
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VU0360172 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
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:

VU03601721310012-12-4VU 0360172VU-0360172mGluRMetabotropic glutamate receptorsPolyphosphoinositidePI hydrolysisCD1 miceInhibitorinhibitorinhibit

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製品名:
VU0360172
製品番号:
HY-120589
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