SB-215505
Based on 1 Customer Validation
SB-215505 is an orally active and subtype-selective 5-HT2B receptor antagonist with pKi values of 8.3, 6.77, 7.66 for 5-HT2B, 5-HT2A, 5-HT2C, respectively. SB-215505 increases wakefulness and motor activity in rats.
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: 98.91%
- CAS 番号: 162100-15-4
- 分子式: C19H16ClN3O
- 分子量:337.80
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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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Help & FAQs
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5-HT 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-HT2A Receptor |
5-HT2B Receptor |
5-HT2C Receptor |
5-HT2B Receptor 8.3 (pKi) |
5-HT2A Receptor 6.77 (pKi) |
5-HT2C Receptor 7.66 (pKi) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO-K1 | IC50 |
13 nM
Compound: SB-215505
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Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
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[PMID: 19307114] |
| CHO-K1 | IC50 |
64 nM
Compound: SB-215505
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Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
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[PMID: 19307114] |
SB-215505 is 30 fold selective for the 5-HT2B over the 5-HT2A receptor, and only marginally selective over the 5-HT2C receptor[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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 weighing 230-260 g[2]
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Dosage:0.1, 0.3 and 1.0 mg/kg
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Administration:IP; two doses (4 days between two doses)
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Result:Dose-dependently increased wakefulness (W) and decreased intermediate stage of sleep (IS), paradoxical sleep (PS), SWS-2.
化学情報
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CAS 番号 162100-15-4
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性状 Solid
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分子量 337.80
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分子式 C19H16ClN3O
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Color Off-white to light brown
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SMILES
O=C(N1CCC2=C1C=C(Cl)C(C)=C2)NC3=C4C=CC=NC4=CC=C3
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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
溶剤 & 溶解度
DMSO : 25 mg/mL (74.01 mM; ultrasonic and warming and heat to 60°C; 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)
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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SDS (393 KB)
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- Deutsch - DE (393 KB)
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- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. C Reavill, et al. Attenuation of haloperidol-induced catalepsy by a 5-HT2C receptor antagonist. Br J Pharmacol. 1999 Feb;126(3):572-4. [Content Brief]
[2]. Sandor Kantor, et al. Increased wakefulness, motor activity and decreased theta activity after blockade of the 5-HT2B receptor by the subtype-selective antagonist SB-215505. J Pharmacol. 2004 Aug;142(8):1332-42. [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 | 2.9603 mL | 14.8017 mL | 29.6033 mL | 74.0083 mL |
| 5 mM | 0.5921 mL | 2.9603 mL | 5.9207 mL | 14.8017 mL | |
| 10 mM | 0.2960 mL | 1.4802 mL | 2.9603 mL | 7.4008 mL | |
| 15 mM | 0.1974 mL | 0.9868 mL | 1.9736 mL | 4.9339 mL | |
| 20 mM | 0.1480 mL | 0.7401 mL | 1.4802 mL | 3.7004 mL | |
| 25 mM | 0.1184 mL | 0.5921 mL | 1.1841 mL | 2.9603 mL | |
| 30 mM | 0.0987 mL | 0.4934 mL | 0.9868 mL | 2.4669 mL | |
| 40 mM | 0.0740 mL | 0.3700 mL | 0.7401 mL | 1.8502 mL | |
| 50 mM | 0.0592 mL | 0.2960 mL | 0.5921 mL | 1.4802 mL | |
| 60 mM | 0.0493 mL | 0.2467 mL | 0.4934 mL | 1.2335 mL |
SB-215505 関連分類
HY-18596 関連分類
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