Ritanserin
Based on 3 publication(s) in Google Scholar
Ritanserin (R 55667) is a highly potent, relatively selective, orally active, long acting antagonist of 5-HT2 receptor, with an IC50 of 0.9 nM, less active on Histamine H1, Dopamine D2, Adrenergic α1, Adrenergic α2 receptors.
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: 99.68%
- CAS 番号: 87051-43-2
- 分子式: C27H25F2N3OS
- 分子量:477.57
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保管条件:
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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 Ritanserin
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Cell Proliferation/Viability Assay
5-HT Receptor アイソフォーム固有の製品をすべて表示
MoreHistamine Receptor アイソフォーム固有の製品をすべて表示
MoreDopamine Receptor アイソフォーム固有の製品をすべて表示
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
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5-HT2 Receptor 0.9 nM (IC50) |
H1 Receptor 35 nM (IC50) |
D2 Receptor 70 nM (IC50) |
Adrenergic α1 97 nM (IC50) |
Adrenergic α2 150 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MDCK | IC50 |
16.7 μM
Compound: R103
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Inhibition of OST-tagged DGKalpha (unknown origin) expressed in MDCK cell homogenates using DAG as substrate measured after 5 mins in presence of [gamma-32P]ATP by TLC analysis
Inhibition of OST-tagged DGKalpha (unknown origin) expressed in MDCK cell homogenates using DAG as substrate measured after 5 mins in presence of [gamma-32P]ATP by TLC analysis
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[PMID: 30611057] |
Ritanserin (R 55667) is a highly potent, relatively selective, long acting antagonist of 5-HT2 receptor, with an IC50 of 0.9 nM, less active on Histamine-H1 (IC50, 35 nM), Dopamine-D2 (IC50, 70 nM), Adrenergic-α1 (IC50, 97 nM), Adrenergic-α2 receptor (IC50, 150 nM)[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 87051-43-2
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性状 Solid
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分子量 477.57
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分子式 C27H25F2N3OS
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Color White to yellow
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SMILES
CC1=C(C(N(C=CS2)C2=N1)=O)CCN(CC/3)CCC3=C(C4=CC=C(F)C=C4)\C5=CC=C(F)C=C5
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別名
R 55667; リタンセリン
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications (3)
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Journal Impact Factor
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Most Recent
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Sci Data
High-throughput drug screening identifies novel therapeutics for Low Grade Serous Ovarian Carcinoma. [Abstract]2024 Sep 19;11(1):1024. PMID: 39300112 -
Prog Neuropsychopharmacol Biol Psychiatry
Baicalein exerts anxiolytic and antinociceptive effects in a mouse model of posttraumatic stress disorder: Involvement of the serotonergic system and spinal delta-opioid receptors. [Abstract]2023 Mar 2:122:110689. PMID: 36462602 -
Thorac Cancer
2023 May;14(13):1179-1191. PMID: 36965165
Ritanserin purchased from MedChemExpress. Usage Cited in: Thorac Cancer. 2023 May;14(13):1179-1191. [Abstract]
Ritanserin (10 mg/mice; injecte; single daily for 15 days) significantly slows the growth of xenograft tumors (xenografts formed from A549 cells) in mice.
溶剤 & 溶解度
DMSO : 25 mg/mL (52.35 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
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 (stored under nitrogen). 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 (stored under nitrogen). 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 (5.23 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. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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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取扱説明書 (2659 KB)
参考文献
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 (stored under nitrogen). 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 | 2.0939 mL | 10.4697 mL | 20.9393 mL | 52.3483 mL |
| 5 mM | 0.4188 mL | 2.0939 mL | 4.1879 mL | 10.4697 mL | |
| 10 mM | 0.2094 mL | 1.0470 mL | 2.0939 mL | 5.2348 mL | |
| 15 mM | 0.1396 mL | 0.6980 mL | 1.3960 mL | 3.4899 mL | |
| 20 mM | 0.1047 mL | 0.5235 mL | 1.0470 mL | 2.6174 mL | |
| 25 mM | 0.0838 mL | 0.4188 mL | 0.8376 mL | 2.0939 mL | |
| 30 mM | 0.0698 mL | 0.3490 mL | 0.6980 mL | 1.7449 mL | |
| 40 mM | 0.0523 mL | 0.2617 mL | 0.5235 mL | 1.3087 mL | |
| 50 mM | 0.0419 mL | 0.2094 mL | 0.4188 mL | 1.0470 mL |
Ritanserin 関連分類
HY-10791 関連分類
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