| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| Other Sizes |
|
Purity: ≥98%
AZD-7325 is a novel, potent and selective GABAA(α2/3) receptor modulator, used for treatment of generalized anxiety disorder. The increases in prolactin levels after administration of AZD7325 at 2 mg and 10 mg doses (difference 7.6% and 10.5%, respectively) did not reach statistical significance, suggesting that doses of AZD7325 or intrinsic efficacy at the α2 and α3 receptor subtypes may have been too low.
| ln Vitro |
AZD7325 displays strong binding affinities on GABAAα1, α2, and α3 (Ki=0.5, 0.3, and 1.3 nM), as well as GABAAα5 (Ki=230 nM), making it a highly selective and high-affinity modulator of the GABAA absorption system [4]. AZD7325 (0–10 μM; 3 days; once daily) causes human hepatocytes from donors HH210, HH215, and HH216, respectively, to express CYP1A2 mRNA at maximum levels of 3.2, 2.1, and 2.5 folds [2]. -10 μM; once daily for three days in a row) induced the production of CYP1A2 and CYP3A4 proteins in human hepatocytes from donor HH210 [2].
|
|---|---|
| ln Vivo |
AZD7325 (Turkish project; 10, 17.8 or 31.6 mg/kg; 30 minutes before induction hyperthermia) enhanced the effectiveness of hyperthermia, with median thresholds in the vehicle group of 42.2°C, 42.8°C (10 mg/kg), and 43.3°C (17.8 mg/kg), as well as 43.4°C (31.6 mg/kg) [3].
|
| Cell Assay |
RT-PCR[2]
Cell Types: Primary human hepatocytes from one female (HH210) and two female males (HH215, HH216) Donor Tested Concentrations: 0.01, 0.1, 1, 10 µM Incubation Duration: 3 consecutive days Experimental Results: Resulted in increased CYP1A2 mRNA expression Western Blot analysis [2] Cell Types: Primary human hepatocytes from donor Tested Concentrations: 0.01, 0.1, 1, 10 µM Incubation Duration: 3 consecutive days Experimental Results: Increased CYP1A2 and CYP3A4 protein levels. |
| Animal Protocol |
Animal/Disease Models: Male and female P18 - P20 F1.Scn1a+/- mice [3]
Doses: 10, 17.8 or 31.6 mg/kg Route of Administration: po (po (oral gavage)) 30 minutes before induction of hyperthermia Experimental Results: In F1.Scn1a+/- mice Hyperthermia-induced seizures are attenuated without sedation. |
| References |
[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.
[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. [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. [4]. AZD7325,Mechanism of action: Gamma-aminobutyric acid receptor A alpha 2 & 3 (GABAAα2,3) positive modulator |
| Molecular Formula |
C19H19FN4O2
|
|---|---|
| Molecular Weight |
354.378167390823
|
| CAS # |
942437-37-8
|
| Related CAS # |
1252802-75-7 (hydrogen sulfate);
|
| SMILES |
O=C(C1=NN=C2C(C3=C(OC)C=CC=C3F)=CC=CC2=C1N)NCCC
|
| InChi Key |
KYDURMHFWXCKMW-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C19H19FN4O2/c1-3-10-22-19(25)18-16(21)12-7-4-6-11(17(12)23-24-18)15-13(20)8-5-9-14(15)26-2/h4-9H,3,10H2,1-2H3,(H2,21,23)(H,22,25)
|
| Chemical Name |
4-amino-8-(2-fluoro-6-methoxyphenyl)-N-propylcinnoline-3-carboxamide
|
| Synonyms |
AZD-7325; AZD 7325; AZD7325.
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~282.18 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.87 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.87 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA