SB-269970 |
Catalog No.GC37599
One-Click Copy Product Info
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SB-269970은 강력하고 선택적인 5-HT₇ 수용체 길항제로 높은 친화력(pKi = 8.9)을 가지고 있다.
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-269970은 강력하고 선택적인 5-HT₇ 수용체 길항제로 높은 친화력(pKi = 8.9)을 가지고 있다. SB-269970은 혈뇌장벽을 통과할 수 있고 5-HT₇ 수용체가 중추신경계 기능에 미치는 영향을 연구에 널리 사용된다[2]. SB-269970은 약리학 연구에서 우울증, 불안장애, 수면장애 등에서 잠재적인 치료적 적용을 탐구하는데 사용된다[3].
SB-269970 (1 µ M;24h) 처리하면 PC-3 세포에서 증식을 억제할 수 있고 세포 사멸 유도 효과와 관련이 있다[4]. SB-269970과 MSX3, 케탄세린을 함께 처리하면 신경모세포종 세포 라인에서 장기적으로 pAKT 발현을 억제할 수 있다[5].
SB-269970(1mg/kg)은 쥐에서 보겔 음용 시험과 상승된 플러스 미로 시험에서 특이적인 항불안 효과를 나타냈다[6]. SB-269970(10과 30mg/kg)은 쥐에서 암페타민 유도한 사육과 선화를 현저하게 감소시켰다[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.
| 세포 실험 [1]: | |
세포 라인 | PC-3 세포 |
제조 방법 | 세포를 1µM SB-269970로 24시간 처리했습니다. 이 후에 MTT 검사를 통해 세포 생존력을 측정했습니다. |
반응 조건 | 1µM; 24시간 동안 |
응용 분야 | SB-269970 처리는 PC-3 세포의 생존력을 감소시킵니다. |
| 동물 실험 [2]: | |
동물 모형 | 수컷 위스타 쥐 |
제조 방법 | SB-269970은 갈등음주검사 (Vogel test)를 시작하기 30분 전에 투여되었습니다. 그리고 5분짜리 실험 세션 동안 받은 충격의 수가 기록되었습니다. |
제형 | 1mg/kg; i.p. |
응용 분야 | 쥐에서 보겔 음용 시험에서 SB-269970은 특이적인 항불안성 효과를 나타냈습니다. |
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)
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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.)