SB 258719
Based on 1 publication(s) in Google Scholar
SB 258719 is a selective 5-HT7 receptor antagonist with high affinity (pKi=7.5) for the receptor. SB 258719 can be used for the research of cancer and neurological disease.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.94%
- No. CAS: 195199-95-2
- Fòrmula: C18H30N2O2S
- Peso molecular:338.51
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Almacenamiento:Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Publications Citing Use of MedChemExpress (MCE) SB 258719
MoreVer todos los productos específicos de isoformas 5-HT Receptor
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Actividad biológica
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5-HT7 Receptor |
5-HT7 Receptor 7.5 (pKi) |
SB 258719 (1, 3 and 10 μM; HEK 293 cells) produces a concentration-related rightward-shift of the 5-CT concentration-response curve with no signifcant alteration in the maximal response to 5-CT[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 Swiss Webster mice (20-25 g)[2].
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Dosage:5-20 mg/kg
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Administration:I.p.
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Result:Significantly attenuated the 5-CT-induced hypothermia.
Chemical Information
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No. CAS 195199-95-2
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Appearance Liquid (Density: 1.075±0.06 g/cm3)
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Peso molecular 338.51
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Fòrmula C18H30N2O2S
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Color Light yellow to orange
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SMILES
O=S(C1=CC=CC(C)=C1)(N(C)[C@H](C)CCN2CCC(C)CC2)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Pure form -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Neurosci Bull
Brain Serotonin Deficiency Impairs Ovarian Reserve Function via the Hypothalamic-Pituitary-Ovarian Axis. [Abstract]2026 May 25. PMID: 42184065
Solvente y solubilidad
DMSO : 250 mg/mL (738.53 mM; Need ultrasonic; 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 6.25 mg/mL (18.46 mM); Clear solution
This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 6.25 mg/mL (18.46 mM); Clear solution
This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (272 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Thomas DR, et al. Functional characterisation of the human cloned 5-HT7 receptor (long form); antagonist profile of SB-258719. Br J Pharmacol. 1998;124(6):1300-1306. [Content Brief]
[2]. Guscott MR, et al. The hypothermic effect of 5-CT in mice is mediated through the 5-HT7 receptor. Neuropharmacology. 2003;44(8):1031-1037. [Content Brief]
[3]. Fatima S, et al. 5-Hydroxytryptamine promotes hepatocellular carcinoma proliferation by influencing β-catenin. Mol Oncol. 2016;10(2):195-212. [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 | 2.9541 mL | 14.7706 mL | 29.5412 mL | 73.8531 mL |
| 5 mM | 0.5908 mL | 2.9541 mL | 5.9082 mL | 14.7706 mL | |
| 10 mM | 0.2954 mL | 1.4771 mL | 2.9541 mL | 7.3853 mL | |
| 15 mM | 0.1969 mL | 0.9847 mL | 1.9694 mL | 4.9235 mL | |
| 20 mM | 0.1477 mL | 0.7385 mL | 1.4771 mL | 3.6927 mL | |
| 25 mM | 0.1182 mL | 0.5908 mL | 1.1816 mL | 2.9541 mL | |
| 30 mM | 0.0985 mL | 0.4924 mL | 0.9847 mL | 2.4618 mL | |
| 40 mM | 0.0739 mL | 0.3693 mL | 0.7385 mL | 1.8463 mL | |
| 50 mM | 0.0591 mL | 0.2954 mL | 0.5908 mL | 1.4771 mL | |
| 60 mM | 0.0492 mL | 0.2462 mL | 0.4924 mL | 1.2309 mL | |
| 80 mM | 0.0369 mL | 0.1846 mL | 0.3693 mL | 0.9232 mL | |
| 100 mM | 0.0295 mL | 0.1477 mL | 0.2954 mL | 0.7385 mL |
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