Sumatriptan
Based on 7 publication(s) in Google Scholar
Sumatriptan (GR 43175) is an orally active 5-HT1 receptor agonist with IC50s of 7.3 nm, 9.3nm and 17.8 nm for 5-HT1D, 5-HT1B and 5-HT1F receptors, respectively. Sumatriptan can be used for migraine headache research.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 99.96%
- CAS No.: 103628-46-2
- 화학식: C14H21N3O2S
- 분자량:295.40
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보관: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
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Sumatriptan
More- ACS Environ Au. 2025 Aug 5;5(6):573-582. [Abstract]
- J Headache Pain. 2024 Oct 30;25(1):187. [Abstract]
- Anal Chem. 2025 Jun 3;97(21):11099-11109. [Abstract]
- Cell Rep Methods. 2023 Oct 23;3(10):100599. [Abstract]
- Headache. 2026 Jun 8. [Abstract]
- Mol Pharmacol. 2023 Nov;104(5):230-238. [Abstract]
- Personalized Medicine Universe. 2019 May.
All 5-HT Receptor Isoforms
More
Biological Activity
제품 설명
IC50 & Target
[1]|
5-HT1D Receptor 17 nM (Ki) |
5-HT1B Receptor |
5-HT1D Receptor |
5-HT1F Receptor |
5-HT1B Receptor 27 nM (Ki) |
5-HT1A Receptor 100 nM (Ki) |
5-HT1D Receptor 7.3 nM (IC50) |
5-HT1B Receptor 9.3 nM (IC50) |
5-HT1F Receptor 17.8 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
14 nM
Compound: Sumatriptan (1)
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Stimulation of [35S]GTP-gamma-S, binding in CHO cells expressing the 5-hydroxytryptamine 1D receptor
Stimulation of [35S]GTP-gamma-S, binding in CHO cells expressing the 5-hydroxytryptamine 1D receptor
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[PMID: 10052975] |
| CHO | IC50 |
11 nM
Compound: Sumatriptan (1)
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Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
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[PMID: 10052975] |
| CHO | IC50 |
6.7 nM
Compound: Sumatriptan (1)
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Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1D receptor stably expressed in CHO cells
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1D receptor stably expressed in CHO cells
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[PMID: 10052975] |
| CHO | EC50 |
14 nM
Compound: Sumatriptan (1)
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Stimulation of [35S]GTP-gamma-S, binding in CHO cells expressing the 5-hydroxytryptamine 1D receptor
Stimulation of [35S]GTP-gamma-S, binding in CHO cells expressing the 5-hydroxytryptamine 1D receptor
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[PMID: 10052976] |
| CHO | IC50 |
11 nM
Compound: Sumatriptan (1)
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Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
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[PMID: 10052976] |
| CHO | IC50 |
6.7 nM
Compound: Sumatriptan (1)
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Displacement of [3H]5-HT binding from human 5-hydroxytryptamine 1D receptor expressed in CHO cells
Displacement of [3H]5-HT binding from human 5-hydroxytryptamine 1D receptor expressed in CHO cells
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[PMID: 10052976] |
| CHO | EC50 |
12 nM
Compound: 1
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Agonist-induced [35S]- GTPgammaS binding in CHO cells stably transfected with 5-hydroxytryptamine 1D receptor
Agonist-induced [35S]- GTPgammaS binding in CHO cells stably transfected with 5-hydroxytryptamine 1D receptor
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[PMID: 10585208] |
| CHO | IC50 |
10 nM
Compound: 1
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Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
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[PMID: 10585208] |
| CHO | IC50 |
6.8 nM
Compound: 1
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Compound was tested for the displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1D receptor stably expressed in CHO cells.
Compound was tested for the displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1D receptor stably expressed in CHO cells.
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[PMID: 10585208] |
| CHO | EC50 |
16 nM
Compound: Sumatriptan
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Measurement of agonist induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with 5-hydroxytryptamine 1D receptor.
Measurement of agonist induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with 5-hydroxytryptamine 1D receptor.
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[PMID: 9357514] |
| CHO | IC50 |
16 nM
Compound: Sumatriptan
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Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
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[PMID: 9357514] |
| CHO | IC50 |
5 nM
Compound: Sumatriptan
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Binding affinity by displacement to human cloned 5-hydroxytryptamine 1D receptor in CHO cells by [3H]5-HT displacement.
Binding affinity by displacement to human cloned 5-hydroxytryptamine 1D receptor in CHO cells by [3H]5-HT displacement.
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[PMID: 9357514] |
| CHO | EC50 |
16 nM
Compound: sumatriptan
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Compound was evaluated for the stimulation of [35S]GTP-gamma-S, binding in CHO cells expressing the 5-hydroxytryptamine 1D receptor.
Compound was evaluated for the stimulation of [35S]GTP-gamma-S, binding in CHO cells expressing the 5-hydroxytryptamine 1D receptor.
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[PMID: 9357515] |
| CHO | IC50 |
16 nM
Compound: sumatriptan
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Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
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[PMID: 9357515] |
| CHO | IC50 |
5 nM
Compound: sumatriptan
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Displacement of [3H]5-HT from human 5-hydroxytryptamine 1D receptor expressed in CHO cells
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1D receptor expressed in CHO cells
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[PMID: 9357515] |
| CHO | EC50 |
38.3 nM
Compound: 1 (Sumatriptan)
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Effective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell lines
Effective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell lines
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[PMID: 9871581] |
| CHO-K1 | EC50 |
77 nM
Compound: sumatriptan
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Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
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[PMID: 8960551] |
| CHO-K1 | EC50 |
30 nM
Compound: Sumatriptan
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Compound was tested for its ability inhibit forskolin-stimulated activity of adenylate cyclase coupled to human 5-hydroxytryptamine 1D receptor beta in CHO-K1 cells; value ranges from 30-70
Compound was tested for its ability inhibit forskolin-stimulated activity of adenylate cyclase coupled to human 5-hydroxytryptamine 1D receptor beta in CHO-K1 cells; value ranges from 30-70
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10.1016/0960-894X(95)00091-7 |
| HEK293 | IC50 |
6.7 μM
Compound: sumatriptan
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Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
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[PMID: 23241029] |
| HeLa | EC50 |
>1000 nM
Compound: Sumatriptan
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Compound was tested for its ability to inhibit forskolin-stimulated activity of adenylate cyclase coupled to human 5-HT 1A receptor in HeLa cells
Compound was tested for its ability to inhibit forskolin-stimulated activity of adenylate cyclase coupled to human 5-HT 1A receptor in HeLa cells
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10.1016/0960-894X(95)00091-7 |
| Oocyte | IC50 |
11 μM
Compound: 17
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Inhibition of human aquaporin 4 M23 isoform expressed in Xenopus laevis oocytes
Inhibition of human aquaporin 4 M23 isoform expressed in Xenopus laevis oocytes
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[PMID: 18182301] |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 103628-46-2
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Appearance Solid
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분자량 295.40
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화학식 C14H21N3O2S
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Color White to off-white
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SMILES
O=S(CC1=CC2=C(NC=C2CCN(C)C)C=C1)(NC)=O
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Synonyms
GR 43175 free base
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선적
Room temperature in continental US; may vary elsewhere.
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보관
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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ACS Environ Au
Machine Learning-Assisted Recognition of Environmental Sulfur-Containing Chemicals in Nontargeted Mass Spectrometry Analysis of Inadequate Mass Resolution. [Abstract]2025 Aug 5;5(6):573-582. PMID: 41277996 -
J Headache Pain
Regional distribution of unbound eletriptan and sumatriptan in the CNS and PNS in rats: implications for a potential central action. [Abstract]2024 Oct 30;25(1):187. PMID: 39478486 -
Anal Chem
Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]2025 Jun 3;97(21):11099-11109. PMID: 40401576 -
Cell Rep Methods
RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]2023 Oct 23;3(10):100599. PMID: 37797618 -
Headache
Inhibiting astrocyte activation is effective in triptan-induced medication-overuse headache model and prolonged hyperalgesia. [Abstract]2026 Jun 8. PMID: 42260315 -
Mol Pharmacol
2023 Nov;104(5):230-238. PMID: 37567783 -
용액&용해도
In Vitro:
DMSO : 50 mg/mL (169.26 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)
In Vivo:
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: ≥ 2.5 mg/mL (8.46 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (8.46 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
In Vivo Dissolution Calculator
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.
순도&문서
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Data Sheet (275 KB)
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SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
- Español - ES (419 KB)
- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Korean - KR (419 KB)
- Portuguese - PT (419 KB)
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Handling Instructions (2659 KB)
References
[1]. S J Peroutka, et al. Sumatriptan (GR 43175) interacts selectively with 5-HT1B and 5-HT1D binding sites. Eur J Pharmacol. 1989 Apr 12;163(1):133-6. [Content Brief]
[2]. K L Dechant, et al. Sumatriptan. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in the acute treatment of migraine and cluster headache. Drugs. 1992 May;43(5):776-98. [Content Brief]
[3]. Razzaque Z, et al. Vasoconstriction in human isolated middle meningeal arteries: determining the contribution of 5-HT1B- and 5-HT1F-receptor activation. Br J Clin Pharmacol. 1999 Jan;47(1):75-82. [Content Brief]
[4]. Bates EA, et al. Sumatriptan alleviates nitroglycerin-induced mechanical and thermal allodynia in mice. Cephalalgia. 2010 Feb;30(2):170-8. [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 | 3.3852 mL | 16.9262 mL | 33.8524 mL | 84.6310 mL |
| 5 mM | 0.6770 mL | 3.3852 mL | 6.7705 mL | 16.9262 mL | |
| 10 mM | 0.3385 mL | 1.6926 mL | 3.3852 mL | 8.4631 mL | |
| 15 mM | 0.2257 mL | 1.1284 mL | 2.2568 mL | 5.6421 mL | |
| 20 mM | 0.1693 mL | 0.8463 mL | 1.6926 mL | 4.2316 mL | |
| 25 mM | 0.1354 mL | 0.6770 mL | 1.3541 mL | 3.3852 mL | |
| 30 mM | 0.1128 mL | 0.5642 mL | 1.1284 mL | 2.8210 mL | |
| 40 mM | 0.0846 mL | 0.4232 mL | 0.8463 mL | 2.1158 mL | |
| 50 mM | 0.0677 mL | 0.3385 mL | 0.6770 mL | 1.6926 mL | |
| 60 mM | 0.0564 mL | 0.2821 mL | 0.5642 mL | 1.4105 mL | |
| 80 mM | 0.0423 mL | 0.2116 mL | 0.4232 mL | 1.0579 mL | |
| 100 mM | 0.0339 mL | 0.1693 mL | 0.3385 mL | 0.8463 mL |
Sumatriptan Related Classifications
HY-B0121B Related Classifications
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