2. GPCR/G Protein Neuronal Signaling
  3. mGluR
  4. AZD-8529

AZD-8529 is a potent, highly selective and orally bioavailable positive allosteric modulator of mGluR2, with an EC50 of 285 nM, and shows no positive allosteric modulator responses at 20-25 M on the mGluR1, 3, 4, 5, 6, 7, and 8 subtypes.

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

AZD-8529 Chemical Structure

AZD-8529 Chemical Structure

CAS No. : 1092453-15-0

Size Price Stock Quantity
Oil + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 161 In-stock
Solution
10 mM * 1 mL in DMSO USD 161 In-stock
Oil
5 mg USD 150 In-stock
10 mg USD 250 In-stock
25 mg USD 550 In-stock
50 mg USD 950 In-stock
100 mg USD 1650 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of AZD-8529:

AZD-8529 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE AZD-8529

View All mGluR Isoform Specific Products:

View All Isoforms
mGluR1 mGluR2 mGluR3 mGluR4 mGluR5 mGluR6 mGluR7 mGluR8 mGluR

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

AZD-8529 is a potent, highly selective and orally bioavailable positive allosteric modulator of mGluR2, with an EC50 of 285 nM, and shows no positive allosteric modulator responses at 20-25 M on the mGluR1, 3, 4, 5, 6, 7, and 8 subtypes.

IC50 & Target[1]

mGluR2

285 nM (EC50)

Cellular Effect
Cell Line Type Value Description References
CHO EC50
195 nM
Compound: 4; AZD8529
Positive allosteric modulation of human mGlu2 receptor expressed in CHO cell membranes assessed as potentiation of glutamate-induced effect incubated for 30 mins prior to [35S]GTPgamma addition measured after 30 mins by scintillation counting method
Positive allosteric modulation of human mGlu2 receptor expressed in CHO cell membranes assessed as potentiation of glutamate-induced effect incubated for 30 mins prior to [35S]GTPgamma addition measured after 30 mins by scintillation counting method
[PMID: 27579727]
In Vitro

AZD-8529 potentiates the effects of glutamate at mGluR2 with an EC50 of 195 nM[1].
AZD-8529 does not elicit antagonist responses on mGluRs at 25 μM[1].

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

AZD-8529 Related Antibodies
In Vivo

AZD-8529 (0.3-mg/kg, i.m.) reduces nicotine priming-induced and cue-induced reinstatement in squirrel monkeys[1].
AZD-8529 (30 mg/kg; i.p.) decreases the increased extracellular dopamine induced by nicotine in accumbens shell of freely-moving rats[1].

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

Animal Model: Sprague-Dawley rats[1]
Dosage: 10 mg/kg, 30 mg/kg
Administration: Intraperitoneal injection; 2 hours before nicotine injections
Result: Decreased the increased extracellular dopamine induced by nicotine (0.4 mg/kg, s.c.) in accumbens shell of freely-moving rats.
Clinical Trial
Molecular Weight

487.47

Formula

C24H24F3N5O3
CAS No.
Appearance

Oil

Color

Off-white to light yellow

SMILES

O=C1C2=C(C)C=C(C3=NC(CN4CCNCC4)=NO3)C=C2CN1CC5=CC=C(OC(F)(F)F)C=C5
Shipping

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

DMSO : 62.5 mg/mL (128.21 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 2.0514 mL 10.2570 mL 20.5141 mL
5 mM 0.4103 mL 2.0514 mL 4.1028 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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 6.25 mg/mL (12.82 mM); Clear solution

    This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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
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 2.0514 mL 10.2570 mL 20.5141 mL 51.2852 mL
5 mM 0.4103 mL 2.0514 mL 4.1028 mL 10.2570 mL
10 mM 0.2051 mL 1.0257 mL 2.0514 mL 5.1285 mL
15 mM 0.1368 mL 0.6838 mL 1.3676 mL 3.4190 mL
20 mM 0.1026 mL 0.5129 mL 1.0257 mL 2.5643 mL
25 mM 0.0821 mL 0.4103 mL 0.8206 mL 2.0514 mL
30 mM 0.0684 mL 0.3419 mL 0.6838 mL 1.7095 mL
40 mM 0.0513 mL 0.2564 mL 0.5129 mL 1.2821 mL
50 mM 0.0410 mL 0.2051 mL 0.4103 mL 1.0257 mL
60 mM 0.0342 mL 0.1710 mL 0.3419 mL 0.8548 mL
80 mM 0.0256 mL 0.1282 mL 0.2564 mL 0.6411 mL
100 mM 0.0205 mL 0.1026 mL 0.2051 mL 0.5129 mL
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AZD-8529 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:

AZD-85291092453-15-0AZD8529AZD 8529mGluRMetabotropic glutamate receptorsmGluR2receptornicotineaddictiontreatmentInhibitorinhibitorinhibit

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