Art. -Nr.: HY-111052

AZD7325

Name: AZD7325
Brand: MedChemExpress
SKU: HY-111052
Price: 80.00 USD
Availability: InStock
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AZD7325 is a potent and orally active partial selective PAM of GABAAα2 and Aα3 receptor (K_i=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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Reinheit : 99.95%
CAS. Nr.: 942437-37-8
Formel: C₁₉H₁₉FN₄O₂
Molecular Weight:354.38

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

AZD7325 Chemical Structure

CAS. Nr.: 942437-37-8

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

AZD7325 is a potent and orally active partial selective PAM of GABAAα2 and Aα3 receptor (K_i=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

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In Vitro

AZD7325 is a high affinity and selective modulator of the GABAA?receptor system, exhibits high binding affinity at GABAAα1,?α2?and?α3?(K_i=0.5, 0.3, and 1.3 nM, respectively), and low at GABAAα5?(K_i=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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .

RT-PCR^[2]

View Protocol

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]

View Protocol

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 942437-37-8
Appearance Solid
Molecular Weight 354.38
Formel C₁₉H₁₉FN₄O₂
Color White to off-white
SMILES

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

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (282.18 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Chen X, et al. The central nervous system effects of the partial GABA-Aα2,3 -selective receptor modulator AZD7325 in comparison with lorazepam in healthy males.Br J Clin Pharmacol. 2014 Dec;78(6):1298-314. [Content Brief]

[2]. Zhou D, et al. A clinical study to assess CYP1A2 and CYP3A4 induction by AZD7325, a selective GABA(A) receptor modulator - an in vitro and in vivo comparison.Br J Clin Pharmacol. 2012 Jul;74(1):98-108. [Content Brief]

[3]. Nomura T, et al. Potentiating α2 subunit containing perisomatic GABAA receptors protects against seizures in a mouse model of Dravet syndrome.J Physiol. 2019 Aug;597(16):4293-4307. [Content Brief]

[4]. AZD7325,Mechanism of action: Gamma-aminobutyric acid receptor A alpha 2 & 3 (GABAAα2,3) positive modulator

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.8218 mL	14.1091 mL	28.2183 mL	70.5457 mL
	5 mM	0.5644 mL	2.8218 mL	5.6437 mL	14.1091 mL
	10 mM	0.2822 mL	1.4109 mL	2.8218 mL	7.0546 mL
	15 mM	0.1881 mL	0.9406 mL	1.8812 mL	4.7030 mL
	20 mM	0.1411 mL	0.7055 mL	1.4109 mL	3.5273 mL
	25 mM	0.1129 mL	0.5644 mL	1.1287 mL	2.8218 mL
	30 mM	0.0941 mL	0.4703 mL	0.9406 mL	2.3515 mL
	40 mM	0.0705 mL	0.3527 mL	0.7055 mL	1.7636 mL
	50 mM	0.0564 mL	0.2822 mL	0.5644 mL	1.4109 mL
	60 mM	0.0470 mL	0.2352 mL	0.4703 mL	1.1758 mL
	80 mM	0.0353 mL	0.1764 mL	0.3527 mL	0.8818 mL
	100 mM	0.0282 mL	0.1411 mL	0.2822 mL	0.7055 mL

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AZD7325

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