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Purity: ≥98%
| Targets |
AZD2066 targets the metabotropic glutamate receptor 5 (mGluR5), a G protein-coupled receptor that plays a key role in modulating synaptic transmission and neuronal excitability in the central nervous system. mGluR5 is activated by glutamate, the primary excitatory neurotransmitter in the brain, and is involved in various physiological processes including learning, memory, pain perception, and anxiety. AZD2066 is a potent, selective antagonist of mGluR5 with IC50 values in the nanomolar range for both rat and human receptors. By blocking mGluR5 activation, AZD2066 modulates glutamatergic signaling and has potential therapeutic applications in pain and neurological disorders.
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| ln Vitro |
In mGlu5/HEK cells, striatum, hippocampal, and cortical cultures, AZD 2066 (1–10 μM) suppresses Ca2+ responses with IC50 values of 27.2±9.1, 3.56±0.52, 96.2±17.8, and 380±78.0 nM, respectively [2]. In mGlu5/HEK cells, AZD 2066 (1–10 μM) prevents the DHPG or Quis effect and suppresses the oscillatory Ca2+ response brought on by the bath solution [2]. Striatal neurons are poorly affected by AZD 2066 (1–10 μM) [2].
AZD2066 demonstrates potent in vitro activity as an mGluR5 antagonist. In mGlu5/HEK cells, the compound suppresses Ca2+ responses with an IC50 of 27.2 nM. In striatal cultures, AZD2066 shows an IC50 of 3.56 nM, while in hippocampal and cortical cultures, it exhibits IC50 values of 96.2 nM and 380 nM, respectively. The compound's potent mGluR5 antagonism makes it a valuable tool for studying the role of mGluR5 in glutamatergic signaling and its involvement in pain, neurological, and psychiatric disorders. AZD2066 inhibits transient lower oesophageal sphincter relaxations (TLESRs) in animals and acid reflux. |
| ln Vivo |
Rats treated orally with AZD 2066 (0.3–30 mg/kg) have distinct effects [1].
AZD2066 has been evaluated in vivo for its effects on pain and reflux. The compound is orally bioavailable and brain-penetrant, making it suitable for oral administration in animal studies. AZD2066 inhibits transient lower oesophageal sphincter relaxations (TLESRs) in animals and acid reflux, showing potential for the treatment of gastro-oesophageal reflux disease. The compound has been used in trials studying the treatment of pain, chronic pain, neuropathic pain, and diabetic neuropathy. AZD2066 displays discriminative effects in rats. Detailed in vivo efficacy data, including specific model results and dosing regimens, are available in the primary literature. |
| Enzyme Assay |
The in vitro receptor binding and functional assay for AZD2066 measures the compound's affinity for and antagonism of the mGluR5 receptor. Radioligand binding assays are performed using membrane preparations from cells expressing human or rat mGluR5 receptors. Varying concentrations of AZD2066 are incubated with the membrane preparation and a radiolabeled mGluR5 ligand. The amount of bound radioligand is measured, and binding affinity is determined. For functional assays, cells expressing mGluR5 are loaded with a fluorescent calcium indicator and treated with varying concentrations of AZD2066 prior to stimulation with glutamate or a selective agonist. The inhibition of agonist-induced calcium influx is measured, and IC50 values are determined. The compound is dissolved in DMSO and diluted in assay buffer. Appropriate positive controls and negative controls are included in each assay run.
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| Cell Assay |
The in vitro cellular assay for AZD2066 is performed using cells expressing mGluR5, such as mGlu5/HEK cells, or primary neuronal cultures from striatum, hippocampus, or cortex. Cells are cultured in appropriate medium and treated with varying concentrations of AZD2066 or vehicle control (DMSO) prior to stimulation with glutamate or a selective mGluR5 agonist. Intracellular calcium levels are measured using fluorescent calcium indicators. The inhibition of agonist-induced calcium responses by AZD2066 is quantified, and IC50 values are determined by fitting dose-response curves (27.2 nM in mGlu5/HEK cells, 3.56 nM in striatal cultures, 96.2 nM in hippocampal cultures, and 380 nM in cortical cultures). The compound's effects on downstream signaling pathways can also be assessed.
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| Animal Protocol |
Animal/Disease Models: Male Wistar rat (weight 240-250 grams) [1]
Doses: 0.03, 0.1, 0.3, 1, 3, 10, 30 mg/kg Route of Administration: Po (60 minutes after administration) Experimental Results:Caused Adequacy and dose-dependent response to AZD9272 is appropriate. In vivo animal experiments with AZD2066 are conducted using rodent models of pain, reflux, or neurological disorders. AZD2066 is administered orally due to its oral bioavailability and brain penetration. For pain models, behavioral tests such as the formalin test, hot plate test, or neuropathic pain models are performed. For reflux studies, the compound's effects on transient lower oesophageal sphincter relaxations (TLESRs) are assessed. The compound's effects on pain-related behaviors or reflux episodes are compared to vehicle-treated controls. Brain penetration is confirmed by measuring compound concentrations in brain tissue. Detailed experimental protocols, including dosing regimens and endpoints, are described in the primary literature. |
| ADME/Pharmacokinetics |
Detailed pharmacokinetic (PK) parameters for AZD2066 are not extensively documented in publicly available sources. The compound is described as orally bioavailable and brain-penetrant. AZD2066 has a molecular weight of 381.82 and a chemical formula of C19H16ClN5O2. The compound is soluble in DMSO for formulation purposes. For in vivo oral administration, AZD2066 is typically formulated using appropriate vehicles to ensure adequate solubility and stability. The compound should be stored under conditions recommended by the manufacturer to maintain stability and prevent degradation. Detailed PK parameters including half-life, clearance, volume of distribution, and maximum concentration (Cmax) are available in the primary literature and should be consulted for specific experimental planning.
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| Toxicity/Toxicokinetics |
Comprehensive toxicological data for AZD2066 are not extensively documented in publicly available sources. As a research-grade compound, AZD2066 is intended for laboratory research purposes only and is not approved for human therapeutic use. Standard laboratory safety practices should be followed when handling this compound, including the use of appropriate personal protective equipment and working in a well-ventilated area. The compound should be stored according to the manufacturer's recommendations to maintain stability and prevent degradation. Comprehensive toxicological profiling (e.g., LD50, maximum tolerated dose, organ-specific toxicity) is not available from the current search results and would require consultation of the primary literature or safety data sheets.
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| References |
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| Additional Infomation |
AZD2066 has been used in research on the treatment and basic science trials of diseases such as pain, chronic pain, reflux, neuropathic pain, and diabetic neuropathy.
AZD2066 is a research compound developed for studying the role of mGluR5 in glutamatergic signaling, pain perception, and neurological disorders. The compound is a potent, selective, orally bioavailable, and brain-penetrant mGluR5 antagonist with IC50 values in the nanomolar range for both rat and human receptors. AZD2066 has been used in trials studying the treatment of pain, chronic pain, reflux episodes, neuropathic pain, and diabetic neuropathy. The compound's ability to inhibit TLESRs and acid reflux supports its potential utility in gastro-oesophageal reflux disease research. AZD2066 is not currently in clinical trials nor approved for therapeutic use; it remains an investigational tool compound for preclinical neuroscience research. AZD2066 is available from various chemical suppliers for research purposes. |
| Molecular Formula |
C19H16CLN5O2
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| Molecular Weight |
381.815642356873
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| Exact Mass |
381.099
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| CAS # |
934282-55-0
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| Related CAS # |
AZD 2066 hydrate
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| PubChem CID |
16041426
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| Appearance |
White to off-white solid powder
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| LogP |
4.325
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
27
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| Complexity |
481
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C[C@H](C1=NOC(=C1)C2=CC(=CC=C2)Cl)OC3=NN=C(N3C)C4=CC=NC=C4
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| InChi Key |
SXWHYTICXCLKDG-GFCCVEGCSA-N
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| InChi Code |
1S/C19H16ClN5O2/c1-12(16-11-17(27-24-16)14-4-3-5-15(20)10-14)26-19-23-22-18(25(19)2)13-6-8-21-9-7-13/h3-12H,1-2H3/t12-/m1/s1
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| Chemical Name |
4-[5-[(1R)-1-[5-(3-Chlorophenyl)-3-isoxazolyl]ethoxy]-4-methyl-4H-1,2,4-triazol-3-yl]pyridine
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| Synonyms |
AZD-2066; AZD 2066; AZD2066.
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.2619 mL | 1.3095 mL | 2.6190 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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