Cyclothiazide
Based on 2 publication(s) in Google Scholar
Cyclothiazide is a positive allosteric modulator of ionotropic AMPA-type glutamate receptors. Cyclothiazide inhibits GABAA receptors. Cyclothiazide is frequently used to produce a fast inhibition of AMPA receptor desensitization and a much slower potentiation of the AMPA current. Cyclothiazide can potentiate responses to kainate in hippocampal neurons. Cyclothiazide has effects on glutamatergic neurotransmission. Cyclothiazide also induces epileptiform EEG activity accompanying behavioral seizures.
For research use only. We do not sell to patients.
- Purity: 99.36%
- CAS No.: 2259-96-3
- Formula: C14H16ClN3O4S2
- Molecular Weight:389.88
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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) Cyclothiazide
MoreAll iGluR Isoforms
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Biological Activity
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AMPA Receptor |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
>100 μM
Compound: CTZ, Cyclothiazide
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Activity at human recombinant GluA2 receptor flop isoform expressed in HEK293 cells assessed as effect on glutamate-induced calcium flux by Fluo-4/AM staining-based fluorescence assay
Activity at human recombinant GluA2 receptor flop isoform expressed in HEK293 cells assessed as effect on glutamate-induced calcium flux by Fluo-4/AM staining-based fluorescence assay
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[PMID: 20096591] |
| HEK293 | EC50 |
13.7 μM
Compound: CTZ, Cyclothiazide
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Activity at human recombinant GluA3 receptor flip isoform expressed in HEK293 cells assessed as effect on glutamate-induced calcium flux by Fluo-4/AM staining-based fluorescence assay
Activity at human recombinant GluA3 receptor flip isoform expressed in HEK293 cells assessed as effect on glutamate-induced calcium flux by Fluo-4/AM staining-based fluorescence assay
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[PMID: 20096591] |
| HEK293 | EC50 |
19.8 μM
Compound: CTZ, Cyclothiazide
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Activity at human recombinant GluA1 receptor flip isoform expressed in HEK293 cells assessed as effect on glutamate-induced calcium flux by Fluo-4/AM staining-based fluorescence assay
Activity at human recombinant GluA1 receptor flip isoform expressed in HEK293 cells assessed as effect on glutamate-induced calcium flux by Fluo-4/AM staining-based fluorescence assay
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[PMID: 20096591] |
| HEK293 | EC50 |
2.24 μM
Compound: CTZ, Cyclothiazide
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Activity at human recombinant GluA2 receptor flip isoform expressed in HEK293 cells assessed as effect on glutamate-induced calcium flux by Fluo-4/AM staining-based fluorescence assay
Activity at human recombinant GluA2 receptor flip isoform expressed in HEK293 cells assessed as effect on glutamate-induced calcium flux by Fluo-4/AM staining-based fluorescence assay
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[PMID: 20096591] |
| HEK293 | EC50 |
3.8 μM
Compound: 2 (cyclothiazide)
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Tested for potentiation towards human iGluR4 receptor expressed in HEK293 cells
Tested for potentiation towards human iGluR4 receptor expressed in HEK293 cells
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[PMID: 11087558] |
| HEK293 | EC50 |
3.91 μM
Compound: CTZ, Cyclothiazide
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Activity at human recombinant GluA4 receptor flip isoform expressed in HEK293 cells assessed as effect on glutamate-induced calcium flux by Fluo-4/AM staining-based fluorescence assay
Activity at human recombinant GluA4 receptor flip isoform expressed in HEK293 cells assessed as effect on glutamate-induced calcium flux by Fluo-4/AM staining-based fluorescence assay
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[PMID: 20096591] |
| HEK293 | EC50 |
3800 nM
Compound: 2, cyclothiazide
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Activity against human GLUR4 flip expressed in HEK293 cells assessed as glutamate-stimulated calcium influx by FLIPR assay
Activity against human GLUR4 flip expressed in HEK293 cells assessed as glutamate-stimulated calcium influx by FLIPR assay
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[PMID: 16879964] |
| HEK293 | EC50 |
7.6 μM
Compound: cyclothiazide
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Agonist activity at human GluA2(Q)i expressed in HEK293 cells assessed as enhancement of glutamate-evoked desensitized current by whole cell patch clamp method
Agonist activity at human GluA2(Q)i expressed in HEK293 cells assessed as enhancement of glutamate-evoked desensitized current by whole cell patch clamp method
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[PMID: 26653877] |
| Oocyte | EC50 |
>76 μM
Compound: CTZ, Cyclothiazide
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Activity at recombinant GluA1A2 receptor flop isoform expressed in Xenopus oocytes assessed as effect on 300 uM glutamate-induced current
Activity at recombinant GluA1A2 receptor flop isoform expressed in Xenopus oocytes assessed as effect on 300 uM glutamate-induced current
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[PMID: 20096591] |
| Oocyte | EC50 |
>91 μM
Compound: CTZ, Cyclothiazide
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Activity at recombinant GluA2A4 receptor flop isoform expressed in Xenopus oocytes assessed as effect on 300 uM glutamate-induced current
Activity at recombinant GluA2A4 receptor flop isoform expressed in Xenopus oocytes assessed as effect on 300 uM glutamate-induced current
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[PMID: 20096591] |
| Oocyte | EC50 |
1 μM
Compound: CTZ, Cyclothiazide
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Agonist activity at recombinant GluA1 receptor flip isoform expressed in Xenopus oocytes
Agonist activity at recombinant GluA1 receptor flip isoform expressed in Xenopus oocytes
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[PMID: 20096591] |
| Oocyte | EC50 |
10 μM
Compound: CTZ, Cyclothiazide
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Activity at recombinant GluA1 receptor flop isoform expressed in Xenopus oocytes co-expressing gamma2-TARP assessed as effect on 10 uM glutamate-induced current by voltage-clamp electrophysiological assay
Activity at recombinant GluA1 receptor flop isoform expressed in Xenopus oocytes co-expressing gamma2-TARP assessed as effect on 10 uM glutamate-induced current by voltage-clamp electrophysiological assay
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[PMID: 20096591] |
| Oocyte | EC50 |
2 μM
Compound: CTZ, Cyclothiazide
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Activity at recombinant GluA1 receptor flip isoform expressed in Xenopus oocytes co-expressing gamma2-TARP assessed as effect on 10 uM glutamate-induced current by voltage-clamp electrophysiological assay
Activity at recombinant GluA1 receptor flip isoform expressed in Xenopus oocytes co-expressing gamma2-TARP assessed as effect on 10 uM glutamate-induced current by voltage-clamp electrophysiological assay
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[PMID: 20096591] |
| Oocyte | EC50 |
5 μM
Compound: CTZ, Cyclothiazide
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Activity at recombinant GluA2A4 receptor flip isoform expressed in Xenopus oocytes assessed as effect on 300 uM glutamate-induced current
Activity at recombinant GluA2A4 receptor flip isoform expressed in Xenopus oocytes assessed as effect on 300 uM glutamate-induced current
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[PMID: 20096591] |
| Oocyte | EC50 |
5.9 μM
Compound: CTZ, Cyclothiazide
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Activity at recombinant GluA4 receptor flip isoform expressed in Xenopus oocytes assessed as effect on 300 uM glutamate-induced current
Activity at recombinant GluA4 receptor flip isoform expressed in Xenopus oocytes assessed as effect on 300 uM glutamate-induced current
|
[PMID: 20096591] |
| Oocyte | EC50 |
6.6 μM
Compound: CTZ, Cyclothiazide
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Activity at recombinant GluA1A2 receptor flip isoform expressed in Xenopus oocytes assessed as effect on 300 uM glutamate-induced current
Activity at recombinant GluA1A2 receptor flip isoform expressed in Xenopus oocytes assessed as effect on 300 uM glutamate-induced current
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[PMID: 20096591] |
| Oocyte | EC50 |
7.1 μM
Compound: 2
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Activity at Wistar rat cortex AMPA receptor expressed in Xenopus laevis oocytes assessed as effect on (S)-AMPA-induced current
Activity at Wistar rat cortex AMPA receptor expressed in Xenopus laevis oocytes assessed as effect on (S)-AMPA-induced current
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[PMID: 17552506] |
| Oocyte | EC50 |
7.6 μM
Compound: Cyclothiazide
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Agonist activity at rat flip iGluR2(Q) expressed in Xenopus laevis oocytes by whole cell patch-clamp method
Agonist activity at rat flip iGluR2(Q) expressed in Xenopus laevis oocytes by whole cell patch-clamp method
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[PMID: 18811139] |
Clyclothiazide (Compound CTZ) (0-1000 μM, 4 s) greatly potentiates AMPA currents dose-dependently and increases the peak AMPA currents by 90-fold at 100 μM (EC50 = 28 μM) in GluR1-HEK cells[1].
Clyclothiazide (100 μM, 0-150 s) inhibits the desensitization in GluR1-HEK cells much faster[1].
Clyclothiazide (30 μM) produces marked and reversible potentiation of responses to kainate in rodent neuron patches[2].
Clyclothiazide (100 μM) produces a leftward shift in the dose-response curve for kainate and reveals a decrease in the EC50 for kainate in rodent neuron patches[2].
Clyclothiazide (100 μM, 240 sec) completely blocks the desensitization evoked by 3 mM kainate in rodent neuron patches[2].
Clyclothiazide (100 μM, 3 min) strongly potentiates the AMPA receptor responses as well as responses to glutamate but to a smaller extent in xenopus oocytes[3].
Clyclothiazide (100 μM) exerts rapid desensitizing responses to glutamate through subunit-modulation in HEK293 cells[3].
Clyclothiazide (5 μM, 48 h) results in abnormal synchronized bursting activities, with high-frequency action potentials overlaying large depolarizing shifts as well as long-term changes of the neural network properties in rodent hippocampal neurons[4].
Clyclothiazide (20-50 μM, 1-2 h) is able to elicit epileptiform activities activities within short-term at high concentrations in rodent hippocampal neurons[4].
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.
Chemical Information
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CAS No. 2259-96-3
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Appearance Solid
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Molecular Weight 389.88
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Formula C14H16ClN3O4S2
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Color White to off-white
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SMILES
O=S(C1=C(Cl)C=C(C2=C1)NC(C3C(C4)C=CC4C3)NS2(=O)=O)(N)=O
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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 (2)
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Journal Impact Factor
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Most Recent
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Sci Adv
2025 Apr 11;11(15):eads5750. PMID: 40215296
Solvent & Solubility
DMSO : 100 mg/mL (256.49 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: ≥ 2.5 mg/mL (6.41 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 (6.41 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.
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 (279 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)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
References
[1]. Fucile S, et al. Effects of cyclothiazide on GluR1/AMPA receptors. Proc Natl Acad Sci U S A. 2006;103(8):2943-2947. [Content Brief]
[2]. Patneau, D. K., et al., (1993). Hippocampal neurons exhibit cyclothiazide-sensitive rapidly desensitizing responses to kainate. The Journal of neuroscience: the official journal of the Society for Neuroscience, 13(8), 3496–3509. [Content Brief]
[3]. Partin, K. M., et al., (1993). Selective modulation of desensitization at AMPA versus kainate receptors by cyclothiazide and concanavalin A. Neuron, 11(6), 1069–1082. [Content Brief]
[4]. Qi, J., et al., (2006). Cyclothiazide induces robust epileptiform activity in rat hippocampal neurons both in vitro and in vivo. The Journal of physiology, 571(Pt 3), 605–618. [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 | 2.5649 mL | 12.8245 mL | 25.6489 mL | 64.1223 mL |
| 5 mM | 0.5130 mL | 2.5649 mL | 5.1298 mL | 12.8245 mL | |
| 10 mM | 0.2565 mL | 1.2824 mL | 2.5649 mL | 6.4122 mL | |
| 15 mM | 0.1710 mL | 0.8550 mL | 1.7099 mL | 4.2748 mL | |
| 20 mM | 0.1282 mL | 0.6412 mL | 1.2824 mL | 3.2061 mL | |
| 25 mM | 0.1026 mL | 0.5130 mL | 1.0260 mL | 2.5649 mL | |
| 30 mM | 0.0855 mL | 0.4275 mL | 0.8550 mL | 2.1374 mL | |
| 40 mM | 0.0641 mL | 0.3206 mL | 0.6412 mL | 1.6031 mL | |
| 50 mM | 0.0513 mL | 0.2565 mL | 0.5130 mL | 1.2824 mL | |
| 60 mM | 0.0427 mL | 0.2137 mL | 0.4275 mL | 1.0687 mL | |
| 80 mM | 0.0321 mL | 0.1603 mL | 0.3206 mL | 0.8015 mL | |
| 100 mM | 0.0256 mL | 0.1282 mL | 0.2565 mL | 0.6412 mL |
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