1. Membrane Transporter/Ion Channel
    Neuronal Signaling
    Metabolic Enzyme/Protease
  2. GABA Receptor
    Cytochrome P450
  3. AZD7325

AZD7325 

Cat. No.: HY-111052
Handling Instructions

AZD7325 is a potent and orally active partial selective PAM of GABAAα2 and Aα3 receptor (Ki=0.3 and 1.3 nM, respectively), and has less antagonistic efficacy at the Aα1 and Aα5 receptor subtypes. AZD7325 is a moderate CYP1A2 and a potent CYP3A4 inducer in vitro. AZD7325 has the potential for the investigation of anxiety and dravet syndrome. PAM: positive allosteric modulator.

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AZD7325 Chemical Structure

AZD7325 Chemical Structure

CAS No. : 942437-37-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 226 In-stock
Estimated Time of Arrival: December 31
10 mg USD 205 In-stock
Estimated Time of Arrival: December 31
50 mg USD 595 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1050 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

AZD7325 is a potent and orally active partial selective PAM of GABAAα2 and Aα3 receptor (Ki=0.3 and 1.3 nM, respectively), and has less antagonistic efficacy at the Aα1 and Aα5 receptor subtypes[1][4]. AZD7325 is a moderate CYP1A2 and a potent CYP3A4 inducer in vitro[2]. AZD7325 has the potential for the investigation of anxiety and dravet syndrome[3]. PAM: positive allosteric modulator.

IC50 & Target[2]

CYP1A2

 

CYP3A4

 

In Vitro

AZD7325 is a high affinity and selective modulator of the GABAA receptor system, exhibits high binding affinity at GABAAα1, α2 and α3 (Ki=0.5, 0.3, and 1.3 nM, respectively), and low at GABAAα5 (Ki=230 nM)[4].
AZD7325 (0-10 µM; 3 consecutive days; once daily) causes a maximal CYP1A2 mRNA expression of 3.2-fold, 2.1-fold, and 2.5-fold in human hepatocytes from donor HH210, HH215, and HH216, respectively[2].
AZD7325 (0-10 µM; 3 consecutive days; once daily) causes CYP1A2 and CYP3A4 protein expression in human hepatocytes from donor HH210[2].

RT-PCR[2]

Cell Line: Primary human hepatocytes from one female (HH210) and two male (HH215, HH216) donors
Concentration: 0.01, 0.1, 1, 10 µM
Incubation Time: 3 consecutive days
Result: Led to increase of CYP1A2 mRNA expression

Western Blot Analysis[2]

Cell Line: Primary human hepatocytes from donors
Concentration: 0.01, 0.1, 1, 10 µM
Incubation Time: 3 consecutive days
Result: Increased CYP1A2 and CYP3A4 protein level.
In Vivo

AZD7325 (oral administration; 10, 17.8 or 31.6 mg/kg; 30 minutes before the induction of hyperthermia) attenuates hyperthermia-induced seizures, shows median thresholds in the treatment groups of 42.8°C for 10 mg/kg, 43.3°C for 17.8 mg/kg, and 43.4°C for 31.6 mg/kg compares to 42.2°C in vehicle group[3].

Animal Model: Male and female P18 - P20 F1.Scn1a+/- mice[3]
Dosage: 10, 17.8 or 31.6 mg/kg
Administration: Oral administration; 30 minutes before the induction of hyperthermia
Result: Attenuated hyperthermia-induced seizures in F1.Scn1a+/- mice with no sedative effect.
Molecular Weight

354.38

Formula

C₁₉H₁₉FN₄O₂

CAS No.

942437-37-8

SMILES

O=C(C1=NN=C2C(C3=C(OC)C=CC=C3F)=CC=CC2=C1N)NCCC

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 : 250 mg/mL (705.46 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8218 mL 14.1091 mL 28.2183 mL
5 mM 0.5644 mL 2.8218 mL 5.6437 mL
10 mM 0.2822 mL 1.4109 mL 2.8218 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 (5.87 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (5.87 mM); Clear solution

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

AZD7325AZD 7325AZD-7325GABA ReceptorCytochrome P450Gamma-aminobutyric acid Receptorγ-Aminobutyric acid ReceptorCYPsDravetsyndromePAMmodulatorCYP1A2anxietysedativeeffectInhibitorinhibitorinhibit

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AZD7325
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