SB-269970 |
Catalog No.GC37599
One-Click Copy Product Info
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SB-269970 is a potent and selective 5-HT7 receptor antagonist, with a high affinity (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 is a potent and selective 5-HT7 receptor antagonist, with a high affinity (pKi = 8.9) [1]. SB-269970 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]. SB-269970 is employed in pharmacological studies to explore its potential therapeutic applications in conditions such as depression, anxiety, and sleep disorders[3].
SB-269970 (1µM; 24h) treatment can inhibit proliferation in PC-3 cells and is associated with an apoptosis-inducing effect[4]. SB-269970 combined with MSX3 and ketanserin treatment can suppress pAKT expression in neuroblastoma cell lines over the long term[5].
SB-269970 (1mg/kg) exerted a specific antianxiety-like effect in the Vogel drinking test and elevated plus-maze test in rats[6]. SB-269970 (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 (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.
| Cell experiment [1]: | |
Cell lines | PC-3 cells |
Preparation Method | Cells were treated with 1µM SB-269970 for 24h. Then the cell viability was detected by MTT assay. |
Reaction Conditions | 1µM; 24h |
Applications | SB-269970 treatment reduces PC-3 cells viability. |
| Animal experiment [2]: | |
Animal models | Male Wistar rats |
Preparation Method | SB-269970 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 | SB-269970 exerted a specific antianxiety-like effect in the Vogel drinking test in rats. |
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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
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.)