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Fig. 1 · Structure
Cat. No.
A13700
CAS No.
2259-96-3
Formula
C14H16ClN3O4S2
Mol. Weight
389.9

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Cyclothiazide

Cat. No. A13700 CAS 2259-96-3

AMPA desensitization inhibitor

Cyclothiazide is a benzothiadiazide that acts as a potentiator of AMPA receptors, positively modulating its response to glutamic acid (EC50 = 3.8 M).

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Biological Activity

Cellular Effect

Cell Line Activity Value Description Reference
HEK293 EC50 > 100 μM 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]
HEK293 EC50 13.7 μM 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 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 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 3.91 μM 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 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 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]
Oocyte EC50 10 μM 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 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 7.6 μM Agonist activity at rat flip iGluR2(Q) expressed in Xenopus laevis oocytes by whole cell patch-clamp method [PMID: 18811139]

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Specifications

Manufacturer Adooq Bioscience
Actions Modulator
CAS Number 2259-96-3
Applications AMPA desensitization inhibitor
Formula C14H16ClN3O4S2
Molecular Weight 389.9
SMILES
C1C2CC(C1C=C2)C3NC4=CC(=C(C=C4S(=O)(=O)N3)S(=O)(=O)N)Cl

Storage & Solubility

In Vitro Solubility

Reported Solubility

No reported solubility data are available for this product.

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

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