Cyclothiazide

Name: Cyclothiazide
Brand: MedChemExpress
SKU: HY-101165
Rating: 5.0 (2 reviews)

Cat. No.: HY-101165 Purity: 99.36%: Data Sheet
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Cyclothiazide is a positive allosteric modulator of ionotropic AMPA-type glutamate receptors. Cyclothiazide inhibits GABA_A 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.

Cyclothiazide Chemical Structure

CAS No. : 2259-96-3

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	Get quote
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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of Cyclothiazide:

Cyclothiazide (Standard) Get quote

2 Publications Citing Use of MCE Cyclothiazide

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AMPA Receptor NMDA Receptor Kainate Receptor

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

AMPA Receptor

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	EC₅₀	13.7 μM Compound: CTZ, Cyclothiazide	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	[PMID: 20096591]
HEK293	EC₅₀	19.8 μM Compound: CTZ, Cyclothiazide	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	[PMID: 20096591]
HEK293	EC₅₀	2.24 μM Compound: CTZ, Cyclothiazide	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	[PMID: 20096591]
HEK293	EC₅₀	3.8 μM Compound: 2 (cyclothiazide)	Tested for potentiation towards human iGluR4 receptor expressed in HEK293 cells Tested for potentiation towards human iGluR4 receptor expressed in HEK293 cells	[PMID: 11087558]
HEK293	EC₅₀	3.91 μM Compound: CTZ, Cyclothiazide	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	[PMID: 20096591]
HEK293	EC₅₀	3800 nM Compound: 2, cyclothiazide	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	[PMID: 16879964]
HEK293	EC₅₀	7.6 μM Compound: cyclothiazide	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	[PMID: 26653877]
HEK293	EC₅₀	> 100 μM Compound: CTZ, Cyclothiazide	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	[PMID: 20096591]
Oocyte	EC₅₀	1 μM Compound: CTZ, Cyclothiazide	Agonist activity at recombinant GluA1 receptor flip isoform expressed in Xenopus oocytes Agonist activity at recombinant GluA1 receptor flip isoform expressed in Xenopus oocytes	[PMID: 20096591]
Oocyte	EC₅₀	10 μM Compound: CTZ, Cyclothiazide	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	[PMID: 20096591]
Oocyte	EC₅₀	2 μM Compound: CTZ, Cyclothiazide	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	[PMID: 20096591]
Oocyte	EC₅₀	5 μM Compound: CTZ, Cyclothiazide	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	[PMID: 20096591]
Oocyte	EC₅₀	5.9 μM Compound: CTZ, Cyclothiazide	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	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	[PMID: 20096591]
Oocyte	EC₅₀	7.1 μM Compound: 2	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	[PMID: 17552506]
Oocyte	EC₅₀	7.6 μM Compound: Cyclothiazide	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	[PMID: 18811139]
Oocyte	EC₅₀	> 76 μM Compound: CTZ, Cyclothiazide	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	[PMID: 20096591]
Oocyte	EC₅₀	> 91 μM Compound: CTZ, Cyclothiazide	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	[PMID: 20096591]

In Vitro

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.

In Vivo

Clyclothiazide (Compound CTZ) (1 M, i.c.v., single dose) results in spontaneous recurrent epileptiform bursts in urethane-anaesthetized rats^[4].

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

Molecular Weight

389.88

Formula

C₁₄H₁₆ClN₃O₄S₂

CAS No.

2259-96-3

Appearance

Solid

Color

White to off-white

SMILES

O=S(C1=C(Cl)C=C(C2=C1)NC(C3C(C4)C=CC4C3)NS2(=O)=O)(N)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.5649 mL	12.8245 mL	25.6489 mL
5 mM	0.5130 mL	2.5649 mL	5.1298 mL
10 mM	0.2565 mL	1.2824 mL	2.5649 mL

View the 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

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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.

Protocol 1

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.
Protocol 2

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.41 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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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

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

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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

Purity: 99.36%

Select Batch:

Data Sheet (279 KB) SDS (394 KB)

COA (253 KB) HNMR (449 KB) RP-HPLC (259 KB) LCMS (94 KB)

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

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

Cyclothiazide Related Classifications

Neurological Disease

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Keywords:

Cyclothiazide2259-96-3iGluRGABA ReceptorIonotropic glutamate receptorsGamma-aminobutyric acid Receptorγ-Aminobutyric acid ReceptorAMPA receptor desensitizationpositive allosteric modulatorcurrent potentiationneuronesInhibitorinhibitorinhibit

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Cyclothiazide

Customer Review

Other Forms of Cyclothiazide:

Cyclothiazide Related Antibodies

2 Publications Citing Use of MCE Cyclothiazide

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All iGluR Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Cyclothiazide Related Antibodies

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Complete Stock Solution Preparation Table

Cyclothiazide Related Classifications

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