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| 5mg |
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Purity: ≥98%
AZD-2066 is a potent, selective, orally bioavailable and brain penetrant antagonist mGlu5 (metabotropic glutamate receptor 5) with IC50 in the nanomolar range for rat and human receptors, respectively. It displays discriminative effects in rats. The discriminative effects of AZD9272 and AZD2066 are similar to those of previously investigated mGluR5 antagonists and dissimilar to those of cocaine, PCP, chlordiazepoxide, and (-)-Δ(9)-THC. The discriminative half-life of AZD9272 is approximately 7-fold longer than for MTEP. These data support and extend previous findings suggesting that mGluR5 antagonism causes psychoactive effects selectively mediated by mGluR5 mechanisms.
| 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].
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| ln Vivo |
Rats treated orally with AZD 2066 (0.3–30 mg/kg) have distinct effects [1].
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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. |
| References |
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| Additional Infomation |
AZD2066 has been used in trials studying the treatment and basic science of Pain, Chronic Pain, Reflux Episodes, Neuropathic Pain, and Diabetic Neuropathy, among others.
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| 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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