1. GPCR/G Protein
    Neuronal Signaling
  2. mGluR
  3. AZD-8529 mesylate

AZD-8529 mesylate 

Cat. No.: HY-107457A Purity: 99.05%
Handling Instructions

AZD-8529 mesylate 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.

For research use only. We do not sell to patients.

AZD-8529 mesylate Chemical Structure

AZD-8529 mesylate Chemical Structure

CAS No. : 1314217-69-0

Size Price Stock Quantity
10 mM * 1  mL in DMSO USD 616 In-stock
Estimated Time of Arrival: December 31
5 mg USD 480 In-stock
Estimated Time of Arrival: December 31
10 mg USD 800 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1700 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2800 In-stock
Estimated Time of Arrival: December 31
100 mg USD 4300 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

AZD-8529 mesylate 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[1].

IC50 & Target[1]

mGluR2

285 nM (EC50)

In Vitro

AZD-8529 mesylate potentiates the effects of glutamate at mGluR2 with an EC50 of 195 nM [1].
AZD-8529 mesylate does not elicit antagonist responses on mGluRs at 25 μM[1].

In Vivo

AZD-8529 mesylate (0.3-mg/kg, i.m.) reduces nicotine priming-induced and cue-induced reinstatement in squirrel monkeys[1].
AZD-8529 mesylate (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.
Molecular Weight

583.58

Formula

C₂₅H₂₈F₃N₅O₆S

CAS No.

1314217-69-0

SMILES

O=C1C2=C(C)C=C(C3=NC(CN4CCNCC4)=NO3)C=C2CN1CC5=CC=C(OC(F)(F)F)C=C5.OS(=O)(C)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 41.67 mg/mL (71.40 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7136 mL 8.5678 mL 17.1356 mL
5 mM 0.3427 mL 1.7136 mL 3.4271 mL
10 mM 0.1714 mL 0.8568 mL 1.7136 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (3.56 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (3.56 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (3.56 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

AZD-8529AZD8529AZD 8529mGluRMetabotropic glutamate receptorsmGluR2receptornicotineaddictiontreatmentInhibitorinhibitorinhibit

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Product Name:
AZD-8529 mesylate
Cat. No.:
HY-107457A
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