ONO-2952
Based on 1 publication(s) in Google Scholar
ONO-2952 is a potent, selective and orally active translocator protein 18 kDa (TSPO) antagonist with Ki of 0.33-9.30 nM for rat and human TSPO. ONO-2952 is more selective for TSPO than other receptors, transporters, ion channels and enzymes. ONO-2952 exerts its anti-stress effects through inhibition of excessive activation of noradrenergic system in the brain without the amnesic effect. ONO-2952 has the potential for irritable bowel syndrome treatment.
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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: 99.51%
- CAS 番号: 895169-20-7
- 分子式: C22H20ClFN2O2
- 分子量:398.86
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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]
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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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MedChemExpress（MCE）の使用を引用している文献 ONO-2952
MoreAdrenergic Receptor アイソフォーム固有の製品をすべて表示
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生物活性
Ki: 0.33-9.30 nM (Rat and human TSPO)[1]
As for its selectivity for TSPO, ONO-2952 at a concentration of 10 μM showed good selectivity for TSPO against 98 off-targets (<50% inhibition). Determination of ONO-2952 Ki or IC50 values for the remaining 35 targets (50% inhibition at 10 μM) reveal Ki values of less than 1 μM only for 3 receptors, i.e. melatonin 2, progesterone B, and adrenergic α2C. The affinity of ONO-2952 for these receptors is at least 59 times lower than that for TSPO. ONO-2952 Ki value for the GABAA receptor is more than 600 times higher than that for TSPO[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
ONO-2952 inhibits both neurosteroid accumulation and noradrenaline release in the brain of rats exposed to acute stress[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 rats (8 weeks old) under conditioned fear stress test[1]
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Dosage:0.03 mg/kg, 0.1 mg/kg, 0.3 mg/kg, 1 mg/kg, 3 mg/kg
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Administration:Oral administration
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Result:Dose-dependently suppressed restraint stress-induced defecation in rats. And suppressed conditioned fear stress-induced freezing behavior in rats.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 895169-20-7
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性状 Solid
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分子量 398.86
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分子式 C22H20ClFN2O2
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Color White to off-white
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SMILES
CC(N([C@H]1C2=CC=C(Cl)C=C2OC)CC3(C4=C1NC5=C4C(F)=CC=C5)CC3)=O
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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 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Phytomedicine
Mechanism of Dihydroartemisinin in activating macrophages to enhance host resistance to malaria. [Abstract]2025 May 26:143:156913. PMID: 40450979
溶剤 & 溶解度
DMSO : 180 mg/mL (451.29 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: 4.5 mg/mL (11.28 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 4.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (45.0 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 (285 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Mitsui K, et al. Anti-stress effects of ONO-2952, a novel translocator protein 18 kDa antagonist, in rats. Neuropharmacology. 2015 Dec;99:51-66. [Content Brief]
[2]. Whitehead WE, et al. Randomised clinical trial: exploratory phase 2 study of ONO-2952 in diarrhoea-predominant irritable bowel syndrome. Aliment Pharmacol Ther. 2017 Jan;45(1):14-26. [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 | 2.5071 mL | 12.5357 mL | 25.0715 mL | 62.6786 mL |
| 5 mM | 0.5014 mL | 2.5071 mL | 5.0143 mL | 12.5357 mL | |
| 10 mM | 0.2507 mL | 1.2536 mL | 2.5071 mL | 6.2679 mL | |
| 15 mM | 0.1671 mL | 0.8357 mL | 1.6714 mL | 4.1786 mL | |
| 20 mM | 0.1254 mL | 0.6268 mL | 1.2536 mL | 3.1339 mL | |
| 25 mM | 0.1003 mL | 0.5014 mL | 1.0029 mL | 2.5071 mL | |
| 30 mM | 0.0836 mL | 0.4179 mL | 0.8357 mL | 2.0893 mL | |
| 40 mM | 0.0627 mL | 0.3134 mL | 0.6268 mL | 1.5670 mL | |
| 50 mM | 0.0501 mL | 0.2507 mL | 0.5014 mL | 1.2536 mL | |
| 60 mM | 0.0418 mL | 0.2089 mL | 0.4179 mL | 1.0446 mL | |
| 80 mM | 0.0313 mL | 0.1567 mL | 0.3134 mL | 0.7835 mL | |
| 100 mM | 0.0251 mL | 0.1254 mL | 0.2507 mL | 0.6268 mL |
ONO-2952 関連分類
HY-111191 関連分類
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