SB-269970 |
Catalog No.GC37599
One-Click Copy Product Info
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SB-269970 es un antagonista del receptor 5-HT7 potente y selectivo, con una alta afinidad (pKi = 8.9)
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 201038-74-6
Sample solution is provided at 25 µL, 10mM.
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SB-269970 es un antagonista del receptor 5-HT7 potente y selectivo, con una alta afinidad (pKi = 8.9) [1]. SB-269970 puede cruzar la barrera hematoencefálica y es ampliamente utilizado en la investigación neurocinómica para estudiar el papel del receptor 5-HT7 en una variedad de funciones del sistema nervioso central [2]. SB-269970 se emplea en estudios farmacológicos para explorar sus posibles aplicaciones terpéuticas en afecciones como la depresión, la ansiedad y los trastornos del sueño [3].
El tratamiento SB-269970 (1µM; 24h) ouede inhibir la proliferación en las células PC-3 y está asociado con un efecto inductor de apoptosis [4]. SB-269970 combinado con MSX3 y ketanserin puede suprimir la expresión de pAKT en líneas celulares de neuroblastoma a largo plazo[5].
SB-269970 (1mg/kg) ejerció un efecto específico similar a la ansiedad en la prueba de consumo de Vogel y la prueba elevada de laberinto plus en ratas [6]. SB-269970 (10 y 30mg/kg) atenuó significativamente la cría y el círculo inducido por anfetaminas en ratas[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 (SB-269970). 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 SB-269970 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 SB-269970 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.
| Experimentos celulares [1]: | |
Líneas celulares | Células PC-3 |
Método de preparación | Las células fueron tratadas con 1µM SB-269970 durante 24h. Luego, la viabilidad celular fue detectada por el ensayo MTT. |
Condiciones de reacción | 1µM; 24h |
Áreas de aplicación | El tratamiento con SB-269970 reduce la viabilidad de las células PC-3. |
| Experimentos con animales [2]: | |
Modelos animales | Ratas Wistar macho |
Método de preparación | Se administró SB-269970 30 minutos antes de la prueba de bebida de conflicto (prueba de Vogel). Luego se registró el número de choques recibidos a lo largo de una sesión experimental de 5 minutos. |
Forma de dosificación | 1mg/kg; i.p. |
Áreas de aplicación | SB-269970 ejerció un efecto antiansiolítico específico en la prueba de consumo de Vogel en ratas. |
References: | |
| Cas No. | 201038-74-6 | SDF | |
| Canonical SMILES | OC1=CC=CC(S(=O)(N2[C@@H](CCN3CCC(C)CC3)CCC2)=O)=C1 | ||
| Formula | C18H28N2O3S | M.Wt | 352.49 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.837 mL | 14.1848 mL | 28.3696 mL |
| 5 mM | 567.4 μL | 2.837 mL | 5.6739 mL |
| 10 mM | 283.7 μL | 1.4185 mL | 2.837 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 2 reference(s) in Google Scholar.)