SB-269970
Based on 7 publication(s) in Google Scholar
SB-269970 is a potent, selective and brain-penetrant 5-HT7 receptor antagonist with a pKi of 8.3. SB-269970 exhibits >50-fold selectivity against other 5-HT receptors.
For research use only. We do not sell to patients.
- Purity: 98.78%
- CAS No.: 201038-74-6
- Formula: C18H28N2O3S
- Molecular Weight:352.49
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) SB-269970
More- Cell Metab. 2025 Dec 17:S1550-4131(25)00495-4. [Abstract]
- Neuron. 2025 Apr 10:S0896-6273(25)00220-X. [Abstract]
- Protein Cell. 2019 Mar;10(3):178-195. [Abstract]
- Cancer Lett. 2024 Aug 1:217150. [Abstract]
- Int J Biol Sci. 2024 Aug 19;20(11):4476-4495. [Abstract]
- J Physiol. 2025 Sep;603(17):4723-4745. [Abstract]
- Authorea. September 19, 2022.
Customer Validation & Images
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In Vivo Efficacy Study
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IF
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WB
All 5-HT Receptor Isoforms
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Biological Activity
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5-HT7 Receptor |
Human 5-HT7 Receptor 8.3 (pKi) |
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Cell Line
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Type | Value | Description | References |
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| HEK293 | IC50 |
3.71 nM
Compound: SB-269970
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Antagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assay
Antagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assay
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[PMID: 27475109] |
| HEK293 | IC50 |
3.71 x 10-3 μM
Compound: SB-269970
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Antagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assay
Antagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assay
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[PMID: 27475109] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL6/J mice[2]
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Dosage:3, 10, 30 mg/kg
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Administration:Intraperitoneal injection; once
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Result:Significantly blocked amphetamine and ketamine-induced hyperactivity.
Chemical Information
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CAS No. 201038-74-6
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Appearance Solid
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Molecular Weight 352.49
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Formula C18H28N2O3S
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Color White to off-white
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SMILES
OC1=CC=CC(S(=O)(N2[C@@H](CCN3CCC(C)CC3)CCC2)=O)=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (7)
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Journal Impact Factor
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Most Recent
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Cell Metab
Serotonin-licensed macrophages potentiate chemoresistance via inositol metabolic crosstalk in ovarian cancer. [Abstract]2025 Dec 17:S1550-4131(25)00495-4. PMID: 41412121 -
Neuron
2025 Apr 10:S0896-6273(25)00220-X. PMID: 40233747 -
Protein Cell
Identification of serotonin 2A receptor as a novel HCV entry factor by a chemical biology strategy. [Abstract]2019 Mar;10(3):178-195. PMID: 29542010 -
Cancer Lett
Serotonylation in tumor-associated fibroblasts contributes to the tumor-promoting roles of serotonin in colorectal cancer. [Abstract]2024 Aug 1:217150. PMID: 39097134
SB-269970 purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2024 Aug 1:217150. [Abstract]
SB-269970 Hydrochloride (SB269970; 5 mg/kg; IP; daily) failed to suppress the growth of shTph1 MC38 tumors in C57BL/6J mice.
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Int J Biol Sci
Chronic Stress-induced Serotonin Impairs Intestinal Epithelial Cell Mitochondrial Biogenesis via the AMPK-PGC-1α Axis. [Abstract]2024 Aug 19;20(11):4476-4495. PMID: 39247815
SB-269970 purchased from MedChemExpress. Usage Cited in: Int J Biol Sci. 2024 Aug 19;20(11):4476-4495. [Abstract]
SB-269970 Hydrochloride (SB269970; 10 μM; 1+24 h) essentially reversed the 5-HT-induced reduction in AMPK phosphorylation and attenuated the 5-HT-induced down-regulation of PGC-1α, TFAM, and VDAC induced by 5-HT in HT-29 cells.
SB-269970 purchased from MedChemExpress. Usage Cited in: Int J Biol Sci. 2024 Aug 19;20(11):4476-4495. [Abstract]
SB-269970 Hydrochloride (SB269970; 30 mg/kg; IP; daily) rescued the reduction in goblet cells in the colon of CRS mice.
SB-269970 purchased from MedChemExpress. Usage Cited in: Int J Biol Sci. 2024 Aug 19;20(11):4476-4495. [Abstract]
SB-269970 Hydrochloride (SB269970; 30 mg/kg; IP; daily) rescued the expression of occludin, claudin-1 and claudin-3 in the colon of CRS mice.
SB-269970 purchased from MedChemExpress. Usage Cited in: Int J Biol Sci. 2024 Aug 19;20(11):4476-4495. [Abstract]
SB-269970 Hydrochloride (SB269970; 30 mg/kg; IP; daily) alleviated the reduction in p-AMPK (T172) levels in the colon of CRS mice, as well as the expression of PGC-1α, TFAM, and VDAC in the colon of CRS mice.
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J Physiol
5-HT7 antagonists confer analgesia via suppression of neurotrophin overproduction in submucosal nerves of mouse models with visceral hypersensitivity. [Abstract]2025 Sep;603(17):4723-4745. PMID: 40757652 -
Solvent & Solubility
DMSO : 100 mg/mL (283.70 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: ≥ 5 mg/mL (14.18 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (14.18 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
Purity & Documentation
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Data Sheet (281 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Hagan JJ, et al. Characterization of SB-269970-A, a selective 5-HT(7) receptor antagonist. Br J Pharmacol. 2000 Jun;130(3):539-48. [Content Brief]
[2]. Roberts C, et al. The effect of SB-269970, a 5-HT(7) receptor antagonist, on 5-HT release from serotonergic terminals and cell bodies. Br J Pharmacol. 2001 Apr;132(7):1574-80. [Content Brief]
[3]. Nikiforuk A, 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. [Content Brief]
[4]. Monti JM, et al. The serotonin 5-HT7 receptor agonist LP-44 microinjected into the dorsal raphe nucleus suppresses REM sleep in the rat. Behav Brain Res. 2008 Aug 22;191(2):184-9. [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 |
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| DMSO | 1 mM | 2.8370 mL | 14.1848 mL | 28.3696 mL | 70.9240 mL |
| 5 mM | 0.5674 mL | 2.8370 mL | 5.6739 mL | 14.1848 mL | |
| 10 mM | 0.2837 mL | 1.4185 mL | 2.8370 mL | 7.0924 mL | |
| 15 mM | 0.1891 mL | 0.9457 mL | 1.8913 mL | 4.7283 mL | |
| 20 mM | 0.1418 mL | 0.7092 mL | 1.4185 mL | 3.5462 mL | |
| 25 mM | 0.1135 mL | 0.5674 mL | 1.1348 mL | 2.8370 mL | |
| 30 mM | 0.0946 mL | 0.4728 mL | 0.9457 mL | 2.3641 mL | |
| 40 mM | 0.0709 mL | 0.3546 mL | 0.7092 mL | 1.7731 mL | |
| 50 mM | 0.0567 mL | 0.2837 mL | 0.5674 mL | 1.4185 mL | |
| 60 mM | 0.0473 mL | 0.2364 mL | 0.4728 mL | 1.1821 mL | |
| 80 mM | 0.0355 mL | 0.1773 mL | 0.3546 mL | 0.8865 mL | |
| 100 mM | 0.0284 mL | 0.1418 mL | 0.2837 mL | 0.7092 mL |
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