2. GPCR/G Protein Neuronal Signaling
  3. mGluR
  4. AZ 12216052

AZ 12216052 is a mGluR8 positive allosteric modulator, and helps mGluR8 modulate signaling inputing to retinal ganglion cells. AZ 12216052 exhibits antianxiety effect.

For research use only. We do not sell to patients.

AZ 12216052 Chemical Structure

AZ 12216052 Chemical Structure

CAS No. : 1290628-31-7

Size Price Stock Quantity
5 mg USD 300 In-stock
10 mg USD 480 In-stock
50 mg   Get quote  
100 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

AZ 12216052 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE AZ 12216052

View All mGluR Isoform Specific Products:

View All Isoforms

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

AZ 12216052 is a mGluR8 positive allosteric modulator, and helps mGluR8 modulate signaling inputing to retinal ganglion cells. AZ 12216052 exhibits antianxiety effect[1][2][3][4].

IC50 & Target

mGlu8

 

In Vitro

mGluR8 may modulates the synaptic inputs to retinal ganglion cells[1].
AZ 12216052 (10 μM) enhances the peak excitatory currents of ON-, OFF- currents in ON-OFF-ganglion cells, with a dependent way on the intensity of the light stimuli[1].
AZ 12216052 shows impact of cell differentiation and (0.01-1 μM; 24-48 h) reduces Dox-induced human neuroblastoma SH-SY5Y cell damage partially[2].
AZ 12216052 stimulates proliferation and attenuates staurosporine (St)- and doxorubicin (Dox)-induced toxicity in UN-SH-SY5Y cells[2].
AZ12216052 (10 μM) enhances glutamate activity of human mGluR8b receptor expressed in GHEK cells[3].

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

AZ 12216052 Related Antibodies

Cell Viability Assay[2]

Cell Line: UN- and RA-SH-SY5Y cells
Concentration: 0.01-1 μM
Incubation Time: 48 hours
Result: Increased cell viability at 0.1 μM, and protected undifferentiated neuroblastoma cells against damaging effects of Iri or Cis.
In Vivo

AZ 12216052 (10 mg/kg; i.p.; 2 h prior to testing) reduces measures of anxiety, without affecting the velocity of the mice[3].
AZ12216052 (10 mg/kg; i.p.; single dose) exhibits remaining anxiolytic effects, might involve mGluR4 in mGluR8−/− mice, as the mGluR4 PAM (Positive Allosteric Modulator) VU 0155041 also reduces measures of anxiety in wild-type mice[4].

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

Animal Model: WT and Apolipoprotein E-deficient (Apoe−/−) mice (C57BL/6J, 2-month-old) in the elevated zero maze[3]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection; singel dose, 2 h prior to testing
Result: Reduced measures of anxiety in the elevated zero maze without affecting the velocity of the mice.
Reduced the acoustic startle response.
Molecular Weight

392.35

Formula

C19H22BrNOS
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(CSCC1=CC=C(C=C1)Br)NC2=CC=C(C(CC)C)C=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (254.87 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 2.5487 mL 12.7437 mL 25.4874 mL
5 mM 0.5097 mL 2.5487 mL 5.0975 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. 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)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.37 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
  • Protocol 2

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

    Solubility: ≥ 2.5 mg/mL (6.37 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). 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 (25.0 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).
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.
Purity & Documentation

Purity: 98.73%

COA (242 KB) HNMR (257 KB) LCMS (93 KB)

Handling Instructions (2659 KB)
References

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. 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 2.5487 mL 12.7437 mL 25.4874 mL 63.7186 mL
5 mM 0.5097 mL 2.5487 mL 5.0975 mL 12.7437 mL
10 mM 0.2549 mL 1.2744 mL 2.5487 mL 6.3719 mL
15 mM 0.1699 mL 0.8496 mL 1.6992 mL 4.2479 mL
20 mM 0.1274 mL 0.6372 mL 1.2744 mL 3.1859 mL
25 mM 0.1019 mL 0.5097 mL 1.0195 mL 2.5487 mL
30 mM 0.0850 mL 0.4248 mL 0.8496 mL 2.1240 mL
40 mM 0.0637 mL 0.3186 mL 0.6372 mL 1.5930 mL
50 mM 0.0510 mL 0.2549 mL 0.5097 mL 1.2744 mL
60 mM 0.0425 mL 0.2124 mL 0.4248 mL 1.0620 mL
80 mM 0.0319 mL 0.1593 mL 0.3186 mL 0.7965 mL
100 mM 0.0255 mL 0.1274 mL 0.2549 mL 0.6372 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

AZ 12216052 Related Classifications

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:

AZ 122160521290628-31-7AZ12216052AZ-12216052mGluRMetabotropic glutamate receptorsantianxietyneuroblastoma cellsretinal ganglion cellsexcitatory currentsON-OFF-ganglion cellsSH-SY5Y cellstaurosporineStdoxorubicinDoxInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
AZ 12216052
Cat. No.:
HY-110122
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

Request for HNMR Report

We have received your request and will respond to you as soon as possible.