AZD7325
Based on 1 Customer Validation
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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 99.95%
- CAS 番号: 942437-37-8
- 分子式: C19H19FN4O2
- 分子量:354.38
-
保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
-
溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
-
HY-101640
TPA 023GABAAalpha2/3 Agonist -
HY-101869
MK-0343GABA(A) Receptor Agonist -
HY-19872
AZD6280GABAA Receptor Modulator -
HY-111052R
AZD7325 (Standard)GABAA Receptor Modulator -
HY-N0197
BaicalinAutophagy Inducer -
HY-103533
GabazineGABAA Antagonist -
HY-121389
HexadecanamideAnti-inflammatory Agent -
HY-N0197R
Baicalin (Standard)Autophagy Inducer -
HY-16716
BasmisanilGABAAα5 NAMs -
HY-107198
(2S)-6-PrenylnaringeninGABAA PAM -
HY-122114
ICA-27243KCNQ2/Q3 Opener -
HY-B0799
Dihydroergotoxine mesylateGABA Receptor Modulator
生物活性
製品説明
IC50 & Target
[2]|
CYP1A2 |
CYP3A4 |
体外実験
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
-
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
-
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.
体内実験
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.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
-
CAS 番号 942437-37-8
-
性状 Solid
-
分子量 354.38
-
分子式 C19H19FN4O2
-
Color White to off-white
-
SMILES
O=C(C1=NN=C2C(C3=C(OC)C=CC=C3F)=CC=CC2=C1N)NCCC
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
体外:
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)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal 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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
-
データシート (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)
-
取扱説明書 (2659 KB)
参考文献
[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]
Complete Stock Solution Preparation Table
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.
| 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 |
AZD7325 関連分類
HY-111052 関連分類
Powered by Bioz