Ralmitaront
Based on 2 publication(s) in Google Scholar
Ralmitaront (RO6889450) is an orally active agonist of trace amine-associated receptor 1 (TAAR1) with a EC50 value of 110.4 nM. Ralmitaront has antipsychotic, cognitively improvement, and antidepressant activity in rodents. Ralmitaront can be used as a neurosuppressant in the study of neuro-related diseases, such as schizophrenia (SCZ), schizoaffective disorder.
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: 99.92%
- CAS 番号: 2133417-13-5
- 分子式: C17H22N4O2
- 分子量:314.38
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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 Ralmitaront
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生物活性
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TAAR1 |
Ralmitaront (0-30 µM, 70 min) displays lower efficacy and slower binding kinetics than Ulotaront at TAAR1, whereas at the 5-HT1AR and the D2 R, Ralmitaront lacks demonstrable activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 2133417-13-5
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性状 Solid
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分子量 314.38
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分子式 C17H22N4O2
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Color White to off-white
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SMILES
O=C(C1=NNC(CC)=C1C)NC2=CC=C([C@H]3CNCCO3)C=C2
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別名
RO6889450
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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 (2)
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Journal Impact Factor
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Most Recent
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Nature
2023 Dec;624(7992):672-681. PMID: 37935376 -
J Med Chem
Rational Design of the First Dual Agonist at Trace Amine-Associated Receptor 1 and 5-HT2C Receptors Based on Binding Pocket Similarity for the Treatment of Schizophrenia and Alzheimer's Disease-Related Psychosis. [Abstract]2025 Apr 10;68(7):7082-7105. PMID: 40159850
溶剤 & 溶解度
DMSO : 100 mg/mL (318.09 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 (7.95 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.95 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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 (273 KB)
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SDS (254 KB)
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- Portuguese - PT (254 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Linda S Brady, et al. Redirecting the revolution: new developments in drug development for psychiatry. Expert Opin Drug Discov. 2019 Dec;14(12):1213-1219. [Content Brief]
[2]. Halff EF, et al. Trace amine-associated receptor 1 (TAAR1) agonism as a new treatment strategy for schizophrenia and related disorders. Trends Neurosci. 2023 Jan;46(1):60-74. [Content Brief]
[3]. Ågren R, et al. In Vitro Comparison of Ulotaront (SEP-363856) and Ralmitaront (RO6889450): Two TAAR1 Agonist Candidate Antipsychotics. Int J Neuropsychopharmacol. 2023 Sep 25;26(9):599-606. [Content Brief]
[4]. Yu J, et al. Elucidating the molecular pharmacology of trace amine-associated receptor 1 to advance antipsychotic drug discovery. Clin Transl Med. 2024 Feb;14(2):e1576. [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 | 3.1809 mL | 15.9043 mL | 31.8086 mL | 79.5216 mL |
| 5 mM | 0.6362 mL | 3.1809 mL | 6.3617 mL | 15.9043 mL | |
| 10 mM | 0.3181 mL | 1.5904 mL | 3.1809 mL | 7.9522 mL | |
| 15 mM | 0.2121 mL | 1.0603 mL | 2.1206 mL | 5.3014 mL | |
| 20 mM | 0.1590 mL | 0.7952 mL | 1.5904 mL | 3.9761 mL | |
| 25 mM | 0.1272 mL | 0.6362 mL | 1.2723 mL | 3.1809 mL | |
| 30 mM | 0.1060 mL | 0.5301 mL | 1.0603 mL | 2.6507 mL | |
| 40 mM | 0.0795 mL | 0.3976 mL | 0.7952 mL | 1.9880 mL | |
| 50 mM | 0.0636 mL | 0.3181 mL | 0.6362 mL | 1.5904 mL | |
| 60 mM | 0.0530 mL | 0.2651 mL | 0.5301 mL | 1.3254 mL | |
| 80 mM | 0.0398 mL | 0.1988 mL | 0.3976 mL | 0.9940 mL | |
| 100 mM | 0.0318 mL | 0.1590 mL | 0.3181 mL | 0.7952 mL |
Ralmitaront 関連分類
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