AZD-2066
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    WARNING: This product is for research use only, not for human or veterinary use.

Hodoodo CAT#: H523115

CAS#: 934282-55-0(AZD-2066)

Description: AZD-2066 is a mGlu5 antagonist. It is orally bioavailable and brain penetrant. It displays discriminative effects in rats.

Chemical Structure

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AZD-2066
CAS# 934282-55-0(AZD-2066)
Instruction

Theoretical Analysis

Hodoodo Cat#: H523115
Name: AZD-2066
CAS#: 934282-55-0(AZD-2066)
Chemical Formula: C19H16ClN5O2
Exact Mass: 381.10
Molecular Weight: 381.820
Elemental Analysis: C, 59.77; H, 4.22; Cl, 9.28; N, 18.34; O, 8.38

Price and Availability

Size Price Availability Quantity
10mg USD 380
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Synonym: AZD-2066; AZD 2066; AZD2066.

IUPAC/Chemical Name: 4-[5-[(1R)-1-[5-(3-Chlorophenyl)-3-isoxazolyl]ethoxy]-4-methyl-4H-1,2,4-triazol-3-yl]pyridine

InChi Key: SXWHYTICXCLKDG-GFCCVEGCSA-N

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

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

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info: Related: 934282-55-0 (AZD-2066) 934338-70-2 (AZD-2066 hydrochloride)

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 381.82 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Jaso BA, Niciu MJ, Iadarola ND, Lally N, Richards EM, Park M, Ballard ED, Nugent AC, Machado-Vieira R, Zarate CA Jr. THERAPEUTIC MODULATION OF GLUTAMATE RECEPTORS IN MAJOR DEPRESSIVE DISORDER. Curr Neuropharmacol. 2016 Mar 21. [Epub ahead of print] PubMed PMID: 26997505.

2: Machado-Vieira R, Henter ID, Zarate CA Jr. New targets for rapid antidepressant action. Prog Neurobiol. 2015 Dec 23. pii: S0301-0082(15)30038-1. doi: 10.1016/j.pneurobio.2015.12.001. [Epub ahead of print] Review. PubMed PMID: 26724279.

3: Dutta A, McKie S, Deakin JF. Ketamine and other potential glutamate antidepressants. Psychiatry Res. 2015 Jan 30;225(1-2):1-13. doi: 10.1016/j.psychres.2014.10.028. Epub 2014 Nov 13. Review. PubMed PMID: 25467702.

4: Swedberg MD, Raboisson P. AZD9272 and AZD2066: selective and highly central nervous system penetrant mGluR5 antagonists characterized by their discriminative effects. J Pharmacol Exp Ther. 2014 Aug;350(2):212-22. doi: 10.1124/jpet.114.215137. Epub 2014 May 29. PubMed PMID: 24876235.

5: Nordmark A, Andersson A, Baranczewski P, Wanag E, Ståhle L. Assessment of interaction potential of AZD2066 using in vitro metabolism tools, physiologically based pharmacokinetic modelling and in vivo cocktail data. Eur J Clin Pharmacol. 2014 Feb;70(2):167-78. doi: 10.1007/s00228-013-1603-8. Epub 2013 Nov 2. PubMed PMID: 24186263.

6: Kågedal M, Cselényi Z, Nyberg S, Raboisson P, Ståhle L, Stenkrona P, Varnäs K, Halldin C, Hooker AC, Karlsson MO. A positron emission tomography study in healthy volunteers to estimate mGluR5 receptor occupancy of AZD2066 - estimating occupancy in the absence of a reference region. Neuroimage. 2013 Nov 15;82:160-9. doi: 10.1016/j.neuroimage.2013.05.006. Epub 2013 May 11. PubMed PMID: 23668965.

7: Hashimoto K, Malchow B, Falkai P, Schmitt A. Glutamate modulators as potential therapeutic drugs in schizophrenia and affective disorders. Eur Arch Psychiatry Clin Neurosci. 2013 Aug;263(5):367-77. doi: 10.1007/s00406-013-0399-y. Epub 2013 Mar 1. Review. PubMed PMID: 23455590.

8: Rohof WO, Lei A, Hirsch DP, Ny L, Astrand M, Hansen MB, Boeckxstaens GE. The effects of a novel metabotropic glutamate receptor 5 antagonist (AZD2066) on transient lower oesophageal sphincter relaxations and reflux episodes in healthy volunteers. Aliment Pharmacol Ther. 2012 May;35(10):1231-42. doi: 10.1111/j.1365-2036.2012.05081.x. Epub 2012 Apr 2. PubMed PMID: 22469098.