AZD8529 free base | CAS#1092453-15-0 | 1314217-69-0

AZD-8529 free base
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 526852

CAS#: 1092453-15-0 (free base)

Description: AZD-8529 is a a positive allosteric modulator at the mGluR2 receptor. AZD8529 decreases Nicotine Self-Administration and Relapse in Squirrel Monkeys. AZD8529 potentiated agonist-induced activation of mGluR2 in the membrane-binding assay and in primate cortex, hippocampus, and striatum. In monkeys, AZD8529 decreased nicotine self-administration at doses (.3-3 mg/kg) that did not affect food self-administration. AZD8529 also reduced nicotine priming- and cue-induced reinstatement of nicotine seeking after extinction of the drug-reinforced responding. In rats, AZD8529 decreased nicotine-induced accumbens dopamine release. The positive allosteric modulators of metabotropic glutamate receptor 2 should be considered for relapse prevention.

Chemical Structure

AZD-8529 free base

CAS# 1092453-15-0 (free base)

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 526852
Name: AZD-8529 free base
CAS#: 1092453-15-0 (free base)
Chemical Formula: C24H24F3N5O3
Exact Mass: 487.18
Molecular Weight: 487.483
Elemental Analysis: C, 59.13; H, 4.96; F, 11.69; N, 14.37; O, 9.85

Price and Availability

Size	Price	Availability
5mg	USD 150	Ready to ship
10mg	USD 250	Ready to ship
25mg	USD 550	Ready to ship
50mg	USD 950	Ready to ship
100mg	USD 1650	Ready to ship
200mg	USD 2650	Ready to Ship
500mg	USD 4650	Ready to Ship
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Related CAS #: 1092453-15-0 (free base) 1314217-69-0 (mesylate) 1344999-56-9 (mesylate hydrate)

Synonym: AZD8529; AZD-8529; AZD 8529.

IUPAC/Chemical Name: 7-methyl-5-[3-(piperazin-1-ylmethyl)-1,2,4-oxadiazol-5-yl]-2-[[4-(trifluoromethoxy)phenyl]methyl]-3H-isoindol-1-one

InChi Key: IPCYZQQFECEHLI-UHFFFAOYSA-N

InChi Code: InChI=1S/C24H24F3N5O3/c1-15-10-17(22-29-20(30-35-22)14-31-8-6-28-7-9-31)11-18-13-32(23(33)21(15)18)12-16-2-4-19(5-3-16)34-24(25,26)27/h2-5,10-11,28H,6-9,12-14H2,1H3

SMILES Code: O=C1N(CC2=CC=C(OC(F)(F)F)C=C2)CC3=C1C(C)=CC(C4=NC(CN5CCNCC5)=NO4)=C3

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

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 CAS# 1092453-15-0 (AZD8529 free base) 1314217-69-0 (AZD8529 hydrochloride salt, 1:1)

Product Data:

Product Data

Certificate of Analysis:

View CoA: current batch, Lot#Y23X05M10

QC Data:

View QC data: current batch, Lot#Y23X05M10

Safety Data Sheet (SDS):

View Safety Data Sheet (SDS)

Instruction:

View handling instruction

Biological target:	AZD-8529 is a positive allosteric modulator of mGluR2, with an EC50 of 285 nM.
In vitro activity:	TBD
In vivo activity:	One-way RM ANOVA showed that AZD8529 significantly decreased reinforcers (F3,93=7.17, p<0.001, Figure 2a) and total ethanol intake (F3,93=7.13, p<0.001, Figure 2b), as well as active lever presses (F3,93=8.30, p<0.001, Figure 2c) while responses on the inactive lever remained low and unaffected (F3,93=1.05, p=0.37, see Supplementary S2). Moreover, post-hoc analyses indicated a significant effect of the low dose of 20 mg/kg on reinforcers, total ethanol intake, and active responses compared with vehicle (p<0.01) but only a trend to reduce alcohol operant self-administration for the high dose of 40 mg/kg (p=0.054 for active lever presses, p=0.076 for reinforcers and p=0.071 for ethanol intake). The vehicle did not affect self-administration compared with baseline (p=0.99 for both reinforcers and lever presses). Thus AZD8529 significantly affected alcohol self-administration, but the magnitude was modest, with a decrease of only 18% compared with vehicle. Reference: Neuropsychopharmacology. 2016 Nov; 41(12): 2932–2940. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5061885/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	62.5	128.21

Preparing Stock Solutions

The following data is based on the product molecular weight 487.48 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.

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:	1. Augier E, Dulman RS, Rauffenbart C, Augier G, Cross AJ, Heilig M. The mGluR2 Positive Allosteric Modulator, AZD8529, and Cue-Induced Relapse to Alcohol Seeking in Rats. Neuropsychopharmacology. 2016 Nov;41(12):2932-2940. doi: 10.1038/npp.2016.107. Epub 2016 Jun 24. PMID: 27339394; PMCID: PMC5061885. 2. Justinova Z, Panlilio LV, Secci ME, Redhi GH, Schindler CW, Cross AJ, Mrzljak L, Medd A, Shaham Y, Goldberg SR. The Novel Metabotropic Glutamate Receptor 2 Positive Allosteric Modulator, AZD8529, Decreases Nicotine Self-Administration and Relapse in Squirrel Monkeys. Biol Psychiatry. 2015 Oct 1;78(7):452-62. doi: 10.1016/j.biopsych.2015.01.014. Epub 2015 Feb 7. PMID: 25802079; PMCID: PMC4529372.
In vitro protocol:	TBD
In vivo protocol:	1. Augier E, Dulman RS, Rauffenbart C, Augier G, Cross AJ, Heilig M. The mGluR2 Positive Allosteric Modulator, AZD8529, and Cue-Induced Relapse to Alcohol Seeking in Rats. Neuropsychopharmacology. 2016 Nov;41(12):2932-2940. doi: 10.1038/npp.2016.107. Epub 2016 Jun 24. PMID: 27339394; PMCID: PMC5061885. 2. Justinova Z, Panlilio LV, Secci ME, Redhi GH, Schindler CW, Cross AJ, Mrzljak L, Medd A, Shaham Y, Goldberg SR. The Novel Metabotropic Glutamate Receptor 2 Positive Allosteric Modulator, AZD8529, Decreases Nicotine Self-Administration and Relapse in Squirrel Monkeys. Biol Psychiatry. 2015 Oct 1;78(7):452-62. doi: 10.1016/j.biopsych.2015.01.014. Epub 2015 Feb 7. PMID: 25802079; PMCID: PMC4529372.

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1: Augier E, Dulman RS, Rauffenbart C, Augier G, Cross AJ, Heilig M. The mGluR2 Positive Allosteric Modulator, AZD8529, and Cue-Induced Relapse to Alcohol Seeking in Rats. Neuropsychopharmacology. 2016 Jul 20. doi: 10.1038/npp.2016.107. [Epub ahead of print] PubMed PMID: 27339394.

2: Litman RE, Smith MA, Doherty JJ, Cross A, Raines S, Gertsik L, Zukin SR. AZD8529, a positive allosteric modulator at the mGluR2 receptor, does not improve symptoms in schizophrenia: A proof of principle study. Schizophr Res. 2016 Apr;172(1-3):152-7. doi: 10.1016/j.schres.2016.02.001. Epub 2016 Feb 26. PubMed PMID: 26922656.

3: Li X, D'Souza MS, Niño AM, Doherty J, Cross A, Markou A. Attenuation of nicotine-taking and nicotine-seeking behavior by the mGlu2 receptor positive allosteric modulators AZD8418 and AZD8529 in rats. Psychopharmacology (Berl). 2016 May;233(10):1801-14. doi: 10.1007/s00213-016-4220-2. Epub 2016 Feb 13. PubMed PMID: 26873083.

4: Caprioli D, Venniro M, Zeric T, Li X, Adhikary S, Madangopal R, Marchant NJ, Lucantonio F, Schoenbaum G, Bossert JM, Shaham Y. Effect of the Novel Positive Allosteric Modulator of Metabotropic Glutamate Receptor 2 AZD8529 on Incubation of Methamphetamine Craving After Prolonged Voluntary Abstinence in a Rat Model. Biol Psychiatry. 2015 Oct 1;78(7):463-73. doi: 10.1016/j.biopsych.2015.02.018. Epub 2015 Feb 23. PubMed PMID: 25861699; PubMed Central PMCID: PMC4546920.

5: Justinova Z, Panlilio LV, Secci ME, Redhi GH, Schindler CW, Cross AJ, Mrzljak L, Medd A, Shaham Y, Goldberg SR. The Novel Metabotropic Glutamate Receptor 2 Positive Allosteric Modulator, AZD8529, Decreases Nicotine Self-Administration and Relapse in Squirrel Monkeys. Biol Psychiatry. 2015 Oct 1;78(7):452-62. doi: 10.1016/j.biopsych.2015.01.014. Epub 2015 Feb 7. PubMed PMID: 25802079; PubMed Central PMCID: PMC4529372.

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