Abecarnil
Based on 1 Customer Validation
Abecarnil (ZK 112119) is a ligand or a partial agonist for benzodiazepine (BZ) receptor. Abecarnil possesses anxiolytic and anticonvulsant properties. Abecarnil can act as a positive allosteric modulator of GABAA receptor. Abecarnil inhibits the binding of the BZ [3H]lormetazepam to rat cerebral cortex membranes, with an IC50 of 0.82 nM. Abecarnil can be used for epilepsy research.
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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: 99.38%
- CAS 番号: 111841-85-1
- 分子式: C24H24N2O4
- 分子量:404.46
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
Abecarnil enhances the binding of t-[35S]butylbicyclophosphorothionate to rat cortical membranes[1].
Abecarnil exhibits a 3- to 6-fold higher affinity to forebrain BZ receptors than Diazepam (DZP)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Abecarnil (0-2.5 mg/kg, IP, once) dose dependently reduces epileptic activity[3].
Abecarnil is effective against sound-induced convulsions in DBA/2 mice, against air blast-induced generalized seizures in gerbils and against myoclonus in baboons Papio papio[4].
Abecarnil is 2-10 times more potent than DZP in most rodent tests of anxiolytic activity, and in reducing locomotor activity in mice and rats thoroughly habituated to the test chamber[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley CD rats (200-250 g)[2]
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Dosage:0.3 mg/kg
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Administration:IP, once, given 30 min before sacrifice
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Result:Failed to change the basal pregnenolone and progesterone, while only slightly decreased THDOC levels, but antagonized the brain neuroactive steroid increase induced by foot shock.
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Animal Model:WAG/Rij rats (male and female, 190-380 g, age 13-19 weeks, 8 rats each group)[3]
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Dosage:0, 0.16, 0.4, 1.0, and 2.5 mg/kg; 1 mL/400 g
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Administration:IP, once
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Result:Reduced the duration of spike-wave discharges and increased immobile behavior. Dose dependently reduced epileptic activity, whether measured as number, mean duration, or total duration of spike-wave discharges. The ED50 for reducing the number of spike-wave discharges in the second hour was 0.4 mg/kg.
化学情報
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CAS 番号 111841-85-1
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性状 Solid
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分子量 404.46
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分子式 C24H24N2O4
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Color White to off-white
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SMILES
O=C(C1=NC=C2NC3=C(C2=C1COC)C=C(OCC4=CC=CC=C4)C=C3)OC(C)C
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別名
ZK 112119
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 100 mg/mL (247.24 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)
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: ≥ 2.5 mg/mL (6.18 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
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データシート (276 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Stephens DN, et al. Abecarnil, a metabolically stable, anxioselective beta-carboline acting at benzodiazepine receptors. J Pharmacol Exp Ther. 1990 Apr;253(1):334-43. [Content Brief]
[2]. Barbaccia ML, et al. Stress-induced increase in brain neuroactive steroids: antagonism by abecarnil. Pharmacol Biochem Behav. 1996 May;54(1):205-10. [Content Brief]
[3]. Coenen AM, et al. Effects of the beta-carboline abecarnil on epileptic activity, EEG, sleep and behavior of rats. Pharmacol Biochem Behav. 1992 Jul;42(3):401-5. [Content Brief]
[4]. Turski L, et al. Anticonvulsant action of the beta-carboline abecarnil: studies in rodents and baboon, Papio papio. J Pharmacol Exp Ther. 1990 Apr;253(1):344-52. [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 |
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| DMSO | 1 mM | 2.4724 mL | 12.3622 mL | 24.7243 mL | 61.8108 mL |
| 5 mM | 0.4945 mL | 2.4724 mL | 4.9449 mL | 12.3622 mL | |
| 10 mM | 0.2472 mL | 1.2362 mL | 2.4724 mL | 6.1811 mL | |
| 15 mM | 0.1648 mL | 0.8241 mL | 1.6483 mL | 4.1207 mL | |
| 20 mM | 0.1236 mL | 0.6181 mL | 1.2362 mL | 3.0905 mL | |
| 25 mM | 0.0989 mL | 0.4945 mL | 0.9890 mL | 2.4724 mL | |
| 30 mM | 0.0824 mL | 0.4121 mL | 0.8241 mL | 2.0604 mL | |
| 40 mM | 0.0618 mL | 0.3091 mL | 0.6181 mL | 1.5453 mL | |
| 50 mM | 0.0494 mL | 0.2472 mL | 0.4945 mL | 1.2362 mL | |
| 60 mM | 0.0412 mL | 0.2060 mL | 0.4121 mL | 1.0302 mL | |
| 80 mM | 0.0309 mL | 0.1545 mL | 0.3091 mL | 0.7726 mL | |
| 100 mM | 0.0247 mL | 0.1236 mL | 0.2472 mL | 0.6181 mL |
Abecarnil 関連分類
HY-105115 関連分類
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