SB269970 HCl
(Synonyms: SB-269970A) 目录号 : GC10769
SB269970 HCl是一种强效且选择性的5-HT7受体拮抗剂，具有高亲和力 (pKi = 8.9)。
Cas No.:261901-57-9
Sample solution is provided at 25 µL, 10mM.
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SB269970 HCl is a potent and selective 5-HT7 receptor antagonist, with a high affinity (pKi = 8.9) [1]. SB269970 HCl can cross the blood-brain barrier and is widely used in neuroscience research to study the role of the 5-HT7 receptor in a variety of central nervous system functions[2]. SB269970 HCl is employed in pharmacological studies to explore its potential therapeutic applications in conditions such as depression, anxiety, and sleep disorders[3].
SB269970 HCl (1µM; 24h) treatment can inhibit proliferation in PC-3 cells and is associated with an apoptosis-inducing effect[4]. SB269970 HCl combined with MSX3 and ketanserin treatment can suppress pAKT expression in neuroblastoma cell lines over the long term[5].
SB269970 HCl (1mg/kg) exerted a specific antianxiety-like effect in the Vogel drinking test and elevated plus-maze test in rats[6]. SB269970 HCl (10 and 30mg/kg) significantly attenuated amphetamine-induced rearing and circling in rats[7].
References:
[1]. Lovell PJ, Bromidge SM, Dabbs S, et al. A novel, potent, and selective 5-HT(7) antagonist: (R)-3-(2-(2-(4-methylpiperidin-1-yl)ethyl)pyrrolidine-1-sulfonyl) phen ol (SB269970 HCl). J Med Chem. 2000 Feb 10;43(3):342-5. doi: 10.1021/jm991151j. PMID: 10669560.
[2]. Nikiforuk A, Kos T, Fijał K, et al. Effects of the selective 5-HT7 receptor antagonist SB269970 HCl and amisulpride on ketamine-induced schizophrenia-like deficits in rats. PLoS One. 2013 Jun 11;8(6):e66695. doi: 10.1371/journal.pone.0066695. PMID: 23776692; PMCID: PMC3679060.
[3]. Guscott M, Bristow LJ, Hadingham K, et al. Genetic knockout and pharmacological blockade studies of the 5-HT7 receptor suggest therapeutic potential in depression. Neuropharmacology. 2005 Mar;48(4):492-502. doi: 10.1016/j.neuropharm.2004.11.015. PMID: 15755477.
[4]. Cinar I, Sirin B, Halici Z, et al. 5-HT7 receptors as a new target for prostate cancer physiopathology and treatment: an experimental study on PC-3 cells and FFPE tissues. Naunyn Schmiedebergs Arch Pharmacol. 2021 Jun;394(6):1205-1213. doi: 10.1007/s00210-021-02051-z. Epub 2021 Feb 2. PMID: 33528589.
[5]. Basaran KE, Korkmaz S, Satır-Basaran G, et al. Short and long-term blockades of adenosine 2A, 5-HT2A, and 5-HT7 receptors induce apoptosis, reduce proliferation, and show differential effects on miR-27b-3p expression in neuroblastoma cell lines. Neuroscience. 2024 Dec 17;563:212-221. doi: 10.1016/j.neuroscience.2024.11.032. Epub 2024 Nov 14. PMID: 39547336.
[6]. Wesołowska A, Nikiforuk A, Stachowicz K, et al. Effect of the selective 5-HT7 receptor antagonist SB 269970 in animal models of anxiety and depression. Neuropharmacology. 2006 Sep;51(3):578-86. doi: 10.1016/j.neuropharm.2006.04.017. Epub 2006 Jul 7. PMID: 16828124.
[7]. Waters KA, Stean TO, Hammond B, et al. Effects of the selective 5-HT(7) receptor antagonist SB269970 HCl in animal models of psychosis and cognition. Behav Brain Res. 2012 Mar 1;228(1):211-8. doi: 10.1016/j.bbr.2011.12.009. Epub 2011 Dec 16. PMID: 22189656.
SB269970 HCl是一种强效且选择性的5-HT7受体拮抗剂，具有高亲和力(pKi=8.9)[1]。SB269970 HCl能够穿过血脑屏障，广泛应用于神经科学研究中，用于探索5-HT7受体在中枢神经系统功能中的作用[2]。SB269970 HCl在药理学研究中被广泛用于探索在抑郁症、焦虑症和睡眠障碍等疾病中的潜在治疗应用[3]。
SB269970 HCl(1µM；24小时)处理可抑制PC-3细胞增殖，并诱导细胞凋亡[4]。SB269970 HCl与MSX3和酮色林联合处理可长期抑制神经母细胞瘤细胞系中的pAKT表达[5]。
SB269970 HCl(1mg/kg)在大鼠Vogel饮水实验和高架十字迷宫实验中表现出特定的抗焦虑作用[6]。SB269970 HCl (10和30mg/kg)处理显著减弱苯丙胺诱导的大鼠直立和转圈行为[7]。
| Cell experiment [1]: | |
Cell lines | PC-3 cells |
Preparation Method | Cells were treated with 1µM SB269970 HCl for 24h. Then the cell viability was detected by MTT assay. |
Reaction Conditions | 1µM; 24h |
Applications | SB269970 HCl treatment reduces PC-3 cells viability. |
| Animal experiment [2]: | |
Animal models | Male Wistar rats |
Preparation Method | SB269970 HCl was given at 30min before the conflict drinking test (Vogel test). Then the number of shocks received throughout a 5min experimental session was recorded. |
Dosage form | 1mg/kg; i.p. |
Applications | SB269970 HCl exerted a specific antianxiety-like effect in the Vogel drinking test in rats. |
References: | |
| Cas No. | 261901-57-9 | SDF | |
| 别名 | SB-269970A | ||
| 化学名 | 3-[(2R)-2-[2-(4-methylpiperidin-1-yl)ethyl]pyrrolidin-1-yl]sulfonylphenol;hydrochloride | ||
| Canonical SMILES | CC1CCN(CC1)CCC2CCCN2S(=O)(=O)C3=CC=CC(=C3)O.Cl | ||
| 分子式 | C18H29ClN2O3S | 分子量 | 388.95 |
| 溶解度 | DMF: 50 mg/ml,DMSO: 50 mg/ml,Ethanol: 5 mg/ml,PBS (pH 7.2): 1 mg/ml | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.571 mL | 12.8551 mL | 25.7102 mL |
| 5 mM | 0.5142 mL | 2.571 mL | 5.142 mL |
| 10 mM | 0.2571 mL | 1.2855 mL | 2.571 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet