ChemicalBook > CAS DataBase List > 7-methyl-5-{3-[(piperazin-1-yl)methyl]-1,2,4-oxadiazol-5-yl}-2-{[4-(trifluoromethoxy)phenyl]methyl}-2,3-dihydro-1H-isoindol-1-one

7-methyl-5-{3-[(piperazin-1-yl)methyl]-1,2,4-oxadiazol-5-yl}-2-{[4-(trifluoromethoxy)phenyl]methyl}-2,3-dihydro-1H-isoindol-1-one

Product Name
7-methyl-5-{3-[(piperazin-1-yl)methyl]-1,2,4-oxadiazol-5-yl}-2-{[4-(trifluoromethoxy)phenyl]methyl}-2,3-dihydro-1H-isoindol-1-one
CAS No.
1092453-15-0
Chemical Name
7-methyl-5-{3-[(piperazin-1-yl)methyl]-1,2,4-oxadiazol-5-yl}-2-{[4-(trifluoromethoxy)phenyl]methyl}-2,3-dihydro-1H-isoindol-1-one
Synonyms
AZD-8529;AZD 8529,AZD8529;AZD-8529 free base;1H-Isoindol-1-one, 2,3-dihydro-7-methyl-5-[3-(1-piperazinylmethyl)-1,2,4-oxadiazol-5-yl]-2-[[4-(trifluoromethoxy)phenyl]methyl]-;7-methyl-5-{3-[(piperazin-1-yl)methyl]-1,2,4-oxadiazol-5-yl}-2-{[4-(trifluoromethoxy)phenyl]methyl}-2,3-dihydro-1H-isoindol-1-one
CBNumber
CB14755525
Molecular Formula
C24H24F3N5O3
Formula Weight
487.47
MOL File
1092453-15-0.mol
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7-methyl-5-{3-[(piperazin-1-yl)methyl]-1,2,4-oxadiazol-5-yl}-2-{[4-(trifluoromethoxy)phenyl]methyl}-2,3-dihydro-1H-isoindol-1-one Property

Boiling point:
650.9±65.0 °C(Predicted)
Density 
1.361±0.06 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
DMSO:62.5(Max Conc. mg/mL);128.21(Max Conc. mM)
pka
8.79±0.10(Predicted)
form 
Oil
color 
Off-white to light yellow
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Safety

WGK Germany 
WGK 3
Storage Class
11 - Combustible Solids
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Danger
Hazard statements

H302Harmful if swallowed

H318Causes serious eye damage

H373May cause damage to organs through prolonged or repeated exposure

Precautionary statements

P260Do not breathe dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P310Immediately call a POISON CENTER or doctor/physician.

P314Get medical advice/attention if you feel unwell.

P330Rinse mouth.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

ChemScene
Product number
CS-0028525
Product name
AZD-8529
Purity
98.43%
Packaging
5mg
Price
$480
Updated
2021/12/16
ChemScene
Product number
CS-0028525
Product name
AZD-8529
Purity
98.43%
Packaging
10mg
Price
$800
Updated
2021/12/16
ChemScene
Product number
CS-0028525
Product name
AZD-8529
Purity
98.43%
Packaging
50mg
Price
$2800
Updated
2021/12/16
DC Chemicals
Product number
DC23437
Product name
AZD-8529
Purity
>98%
Packaging
100mg
Price
$650
Updated
2021/12/16
DC Chemicals
Product number
DC23437
Product name
AZD-8529
Purity
>98%
Packaging
250mg
Price
$1100
Updated
2021/12/16
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7-methyl-5-{3-[(piperazin-1-yl)methyl]-1,2,4-oxadiazol-5-yl}-2-{[4-(trifluoromethoxy)phenyl]methyl}-2,3-dihydro-1H-isoindol-1-one Chemical Properties,Usage,Production

Uses

AZD-8529 is a potent, highly selective and orally bioavailable positive allosteric modulator of mGluR2, with an EC50 of 285 nM, and shows no positive allosteric modulator responses at 20-25 M on the mGluR1, 3, 4, 5, 6, 7, and 8 subtypes.

Biological Activity

AZD8529 is a selective metabotropic glutamate receptor 2 (mGluR2) positive allosteric modulator (PAM) th at potentiates DCG-IV-induced GTPγS binding to membrane from human mGluR2, but not mGluR1/3/4/5/6/7/8, CaR/Gqi5 fusion-expressing HEK293 cells (EC50/Emax = 285 nM/59.9%) with no mGluR agonist/antagonist activity and little or no affinity toward a panel of 50 other receptors. AZD8529 is shown to reduce nicotine self-administration and cue-induced reinstatement of nicotine-seeking responses in squirrel monkeys (0.3-10 mg/kg i.m.) and rats (1.75-58.3 mg/kg) as well as cue-induced methamphetamine seeking in rats (20 and 40 mg/kg s.c.) in vivo.

in vivo

AZD-8529 (0.3-mg/kg, i.m.) reduces nicotine priming-induced and cue-induced reinstatement in squirrel monkeys[1].
AZD-8529 (30 mg/kg; i.p.) decreases the increased extracellular dopamine induced by nicotine in accumbens shell of freely-moving rats[1].

Animal Model:Sprague-Dawley rats[1]
Dosage:10 mg/kg, 30 mg/kg
Administration:Intraperitoneal injection; 2 hours before nicotine injections
Result:Decreased the increased extracellular dopamine induced by nicotine (0.4 mg/kg, s.c.) in accumbens shell of freely-moving rats.

IC 50

mGluR2: 285 nM (EC50)

References

[1] Justinova Z, et al. 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

7-methyl-5-{3-[(piperazin-1-yl)methyl]-1,2,4-oxadiazol-5-yl}-2-{[4-(trifluoromethoxy)phenyl]methyl}-2,3-dihydro-1H-isoindol-1-one Preparation Products And Raw materials

Raw materials

Preparation Products

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7-methyl-5-{3-[(piperazin-1-yl)methyl]-1,2,4-oxadiazol-5-yl}-2-{[4-(trifluoromethoxy)phenyl]methyl}-2,3-dihydro-1H-isoindol-1-one Suppliers

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1092453-15-0, 7-methyl-5-{3-[(piperazin-1-yl)methyl]-1,2,4-oxadiazol-5-yl}-2-{[4-(trifluoromethoxy)phenyl]methyl}-2,3-dihydro-1H-isoindol-1-oneRelated Search:


  • 7-methyl-5-{3-[(piperazin-1-yl)methyl]-1,2,4-oxadiazol-5-yl}-2-{[4-(trifluoromethoxy)phenyl]methyl}-2,3-dihydro-1H-isoindol-1-one
  • AZD-8529
  • 1H-Isoindol-1-one, 2,3-dihydro-7-methyl-5-[3-(1-piperazinylmethyl)-1,2,4-oxadiazol-5-yl]-2-[[4-(trifluoromethoxy)phenyl]methyl]-
  • AZD-8529 free base
  • AZD 8529,AZD8529
  • 1092453-15-0
  • C24H24F3N5O3