Cat. No.: HY-B0121B

Sumatriptan

(Synonyms: GR 43175 free base)

7 Cited Publications

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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-HT_1D, 5-HT_1B and 5-HT_1F receptors, respectively. Sumatriptan can be used for migraine headache research.

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Pureté: 99.96%
CAS No.: 103628-46-2
Formule: C₁₄H₂₁N₃O₂S
Masse moléculaire:295.40

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Sumatriptan Chemical Structure

CAS No.: 103628-46-2

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vivo
Chemical Information
Publications (7)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[1]

5-HT_1D Receptor

17 nM (Ki)

5-HT_1B Receptor

5-HT_1D Receptor

5-HT_1F Receptor

5-HT_1B Receptor

27 nM (Ki)

5-HT_1A Receptor

100 nM (Ki)

5-HT_1D Receptor

7.3 nM (IC₅₀)

5-HT_1B Receptor

9.3 nM (IC₅₀)

5-HT_1F Receptor

17.8 nM (IC₅₀)

Voir tous les produits spécifiques à Isoform 5-HT Receptor :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	14 nM Compound: Sumatriptan (1)	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	[PMID: 10052975]
CHO	IC₅₀	11 nM Compound: Sumatriptan (1)	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	[PMID: 10052975]
CHO	IC₅₀	6.7 nM Compound: Sumatriptan (1)	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	[PMID: 10052975]
CHO	EC₅₀	14 nM Compound: Sumatriptan (1)	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	[PMID: 10052976]
CHO	IC₅₀	11 nM Compound: Sumatriptan (1)	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.	[PMID: 10052976]
CHO	IC₅₀	6.7 nM Compound: Sumatriptan (1)	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	[PMID: 10052976]
CHO	EC₅₀	12 nM Compound: 1	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	[PMID: 10585208]
CHO	IC₅₀	10 nM Compound: 1	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.	[PMID: 10585208]
CHO	IC₅₀	6.8 nM Compound: 1	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.	[PMID: 10585208]
CHO	EC₅₀	16 nM Compound: Sumatriptan	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.	[PMID: 9357514]
CHO	IC₅₀	16 nM Compound: Sumatriptan	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.	[PMID: 9357514]
CHO	IC₅₀	5 nM Compound: Sumatriptan	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.	[PMID: 9357514]
CHO	EC₅₀	16 nM Compound: sumatriptan	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.	[PMID: 9357515]
CHO	IC₅₀	16 nM Compound: sumatriptan	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	[PMID: 9357515]
CHO	IC₅₀	5 nM Compound: sumatriptan	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	[PMID: 9357515]
CHO	EC₅₀	38.3 nM Compound: 1 (Sumatriptan)	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	[PMID: 9871581]
CHO-K1	EC₅₀	77 nM Compound: sumatriptan	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	[PMID: 8960551]
CHO-K1	EC₅₀	30 nM Compound: Sumatriptan	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	10.1016/0960-894X(95)00091-7
HEK293	IC₅₀	6.7 μM Compound: sumatriptan	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	[PMID: 23241029]
HeLa	EC₅₀	>1000 nM Compound: Sumatriptan	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	10.1016/0960-894X(95)00091-7
Oocyte	IC₅₀	11 μM Compound: 17	Inhibition of human aquaporin 4 M23 isoform expressed in Xenopus laevis oocytes Inhibition of human aquaporin 4 M23 isoform expressed in Xenopus laevis oocytes	[PMID: 18182301]

In Vivo

Sumatriptan (600 μg/kg, i.p. or 0.06 μg in 5 μL, i.t.) reverses nitroglycerin-induced thermal hypersensitivity in mice^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 103628-46-2
Appearance Solid
Masse moléculaire 295.40
Formule C₁₄H₂₁N₃O₂S
Color White to off-white
SMILES

O=S(CC1=CC2=C(NC=C2CCN(C)C)C=C1)(NC)=O
Synonyms

GR 43175 free base
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

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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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

G α Protein Signaling Bias at Serotonin 1A Receptor. [Abstract]

2023 Nov;104(5):230-238. PMID: 37567783
Personalized Medicine Universe

2019 May.

Solvant et solubilité

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.3852 mL

16.9262 mL

33.8524 mL

5 mM

0.6770 mL

3.3852 mL

6.7705 mL

10 mM

0.3385 mL

1.6926 mL

3.3852 mL

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.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (8.46 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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g
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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+
%
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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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (275 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
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MS (2659 KB)
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IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Sumatriptan

7 Cited Publications

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Sumatriptan

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Publications Citing Use of MedChemExpress (MCE) Sumatriptan

Voir tous les produits spécifiques à Isoform 5-HT Receptor

Activité biologique

Chemical Information

Publications (7)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Sumatriptan

NMPA-Approved Drug Library

Orally Active Compound Library

Neurotransmitter Receptor Compound Library

FDA Approved & Pharmacopeial Drug Library

Anti-Alzheimer's Disease Compound Library

Anti-Obesity Compound Library

Pediatric Drug Library

Antidepressant Compound Library

5-HT Receptor Compound Library

Human Metabolite Library

Coagulation and Anti-coagulation Compound Library

Off-patent Drug Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

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Mass Spectrometry Human Metabolite Library

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Neuronal Signaling Compound Library

FDA-Approved Drug Library

Drug Repurposing Compound Library

Publications Citing Use of MedChemExpress (MCE) Sumatriptan

Voir tous les produits spécifiques à Isoform 5-HT Receptor

Activité biologique

Chemical Information

Publications (7)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Sumatriptan Related Classifications

HY-B0121B Related Classifications