2. GPCR/G Protein Neuronal Signaling Membrane Transporter/Ion Channel Protein Tyrosine Kinase/RTK
  3. mGluR Calcium Channel Trk Receptor
  4. AZD 2066

AZD-2066 is a selective, orally active and blood-brain barrier-permeating mGluR5 antagonist. AZD 2066 activates the BDNF/trkB signaling pathway. AZD 2066 can be used in the research of neuropathic pain, major depressive disorder and gastroesophageal reflux disease.

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

AZD 2066 Chemical Structure

AZD 2066 Chemical Structure

CAS No. : 934282-55-0

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Based on 1 publication(s) in Google Scholar

Other Forms of AZD 2066:

AZD 2066 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE AZD 2066

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mGluR1 mGluR2 mGluR3 mGluR4 mGluR5 mGluR6 mGluR7 mGluR8 mGluR

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N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

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TrkA TrkB TrkC Trk

  • Biological Activity

  • Purity & Documentation

  • References

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Description

AZD-2066 is a selective, orally active and blood-brain barrier-permeating mGluR5 antagonist. AZD 2066 activates the BDNF/trkB signaling pathway. AZD 2066 can be used in the research of neuropathic pain, major depressive disorder and gastroesophageal reflux disease[1][2][3][5].

IC50 & Target[1]

mGluR5

 

In Vitro

AZD 2066 (1-10 μM) inhibits Ca2+ response, with IC50s of 27.2, 3.56, 96.2, and 380 nM in mGlu5/HEK cells and striatal, hippocampal, and cortical cultures respectively[4].
AZD 2066 (1-10 μM) inhibits the oscillatory Ca2+ response which induced by bath application of DHPG (HY-12598A), and blocks either DHPG or Quis effects in mGlu5/HEK cells[4].

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

AZD 2066 Related Antibodies
In Vivo

AZD 2066 (0.3-30 mg/kg, p.o., 60 min) shows discriminative effects in rats[2].
AZD-2066 (10 µM, perfusion of brain slide) alleviates dihydroxyphenylglycine (DHPG)-facilitated long-term depression (LTD) expression in chronic social defeat stress (CSDS)-treated mice via BDNF/trkB signaling pathway[5].
AZD-2066 (5 mg/kg, i.p., 2 × 12 h) alleviates chronic social defeat stress (CSDS)-induced depressive behaviors in mice[5].

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

Animal Model: Male Wistar rats (weighing 240-250 g)[2]
Dosage: 0.03, 0.1, 0.3, 1, 3, 10, 30 mg/kg
Administration: Oral gavage (p.o.)
Result: Caused full and dose-dependent AZD9272-appropriate responding.
Animal Model: Depressive model (C57BL/6 mice were subjected to physical defeats that were generated by a CD-1 aggressor for 5 min every day for 10 days)[5]
Dosage: 5 mg/kg
Administration: Intraperitoneal injection (i.p.), 2 × 12 h
Result: Increased social interaction ratio.
Reversed time spent in interaction zone.
Increased sucrose preference scores.
Clinical Trial
Molecular Weight

381.82

Formula

C19H16ClN5O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CN1C(C2=CC=NC=C2)=NN=C1O[C@@H](C3=NOC(C4=CC(Cl)=CC=C4)=C3)C
Shipping

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

DMSO : 2 mg/mL (5.24 mM; Need ultrasonic and warming; 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 2.6190 mL 13.0952 mL 26.1904 mL
5 mM 0.5238 mL 2.6190 mL 5.2381 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.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.8%

SDS (557 KB)

COA (246 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 2.6190 mL 13.0952 mL 26.1904 mL 65.4759 mL
5 mM 0.5238 mL 2.6190 mL 5.2381 mL 13.0952 mL
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AZD 2066 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 2066934282-55-0AZD2066AZD-2066mGluRCalcium ChannelTrk ReceptorMetabotropic glutamate receptorsCa2+ channelsCa channelsTropomyosin related kinase receptorMDDNeuropathic painmGlu5/HEK cellDiscriminativeCSDSDepressive behaviors.Inhibitorinhibitorinhibit

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