AZD-9272
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 523125

CAS#: 327056-26-8

Description: AZD-9272 is a potent and selective mGlu5 antagonist (IC50 values are 2.6 and 7.6 nM for rat and human receptors, respectively). It exhibits >3900-fold selectivity for mGlu5 over other mGlu receptors. AZD-9272 displays discriminative effects in rats. This drug is orally bioavailable and brain penetrant.

Chemical Structure

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AZD-9272
CAS# 327056-26-8
Instruction

Theoretical Analysis

MedKoo Cat#: 523125
Name: AZD-9272
CAS#: 327056-26-8
Chemical Formula: C14H6F2N4O
Exact Mass: 284.05
Molecular Weight: 284.230
Elemental Analysis: C, 59.16; H, 2.13; F, 13.37; N, 19.71; O, 5.63

Price and Availability

Size Price Availability Quantity
10mg USD 340
25mg USD 670
50mg USD 1120
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Synonym: AZD-9272; AZD 9272; AZD9272.

IUPAC/Chemical Name: 3-Fluoro-5-[3-(5-fluoro-2-pyridinyl)-1,2,4-oxadiazol-5-yl]benzonitrile

InChi Key: RBSPCALDSNXWEP-UHFFFAOYSA-N

InChi Code: InChI=1S/C14H6F2N4O/c15-10-1-2-12(18-7-10)13-19-14(21-20-13)9-3-8(6-17)4-11(16)5-9/h1-5,7H

SMILES Code: N#CC1=CC(C2=NC(C3=NC=C(F)C=C3)=NO2)=CC(F)=C1

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:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 284.23 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: 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.

2: Kalliomäki J, Huizar K, Kågedal M, Hägglöf B, Schmelz M. Evaluation of the effects of a metabotropic glutamate receptor 5-antagonist on electrically induced pain and central sensitization in healthy human volunteers. Eur J Pain. 2013 Nov;17(10):1465-71. doi: 10.1002/j.1532-2149.2013.00327.x. Epub 2013 May 6. PubMed PMID: 23650072.

3: Andersson JD, Seneca N, Truong P, Wensbo D, Raboisson P, Farde L, Halldin C. Palladium mediated ¹¹C-cyanation and characterization in the non-human primate brain of the novel mGluR5 radioligand [¹¹C]AZD9272. Nucl Med Biol. 2013 May;40(4):547-53. doi: 10.1016/j.nucmedbio.2012.12.012. Epub 2013 Mar 28. PubMed PMID: 23541825.

4: Raboisson P, Breitholtz-Emanuelsson A, Dahllöf H, Edwards L, Heaton WL, Isaac M, Jarvie K, Kers A, Minidis AB, Nordmark A, Sheehan SM, Slassi A, Ström P, Terelius Y, Wensbo D, Wilson JM, Xin T, McLeod DA. Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development. Bioorg Med Chem Lett. 2012 Nov 15;22(22):6974-9. doi: 10.1016/j.bmcl.2012.08.100. Epub 2012 Sep 21. PubMed PMID: 23046966.

5: Kågedal M, Cselényi Z, Nyberg S, Jönsson S, Raboisson P, Stenkrona P, Hooker AC, Karlsson MO. Non-linear mixed effects modelling of positron emission tomography data for simultaneous estimation of radioligand kinetics and occupancy in healthy volunteers. Neuroimage. 2012 Jul 16;61(4):849-56. doi: 10.1016/j.neuroimage.2012.02.085. Epub 2012 Mar 9. PubMed PMID: 22425672.