GYKI 53655 hydrochloride
Based on 1 publication(s) in Google Scholar
GYKI 53655 (LY300168) hydrochloride is an α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) antagonist.
For research use only. We do not sell to patients.
- Purity: 98.37%
- CAS No.: 143692-48-2
- Formula: C19H21ClN4O3
- Molecular Weight:388.85
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) GYKI 53655 hydrochloride
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Biological Activity
AMPA[1]
GYKI 53655 (LY300168) hydrochloride inhibits α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) (10 μM)-induced responses with IC50 value of 5.9±0.1 μM. GYKI 53655 hydrochloride inhibits AMPA (10 μM) responses in recombinant G1uR4 expressing HEK293 cells with IC50 value of 4.6±0.4 μM. Using 3 μM cyclothiazide the inhibition produced by GYKI 53655 hydrochloride is 79±2% (n=4 cells). GYKI 53655 hydrochloride produces only small inhibitions of kainate-induced currents at 30 μM and inhibits kainate-induced currents at a concentration of 100 μM by 12±2 (n=4) and 18±4 (n=4), respectively. GYKI 53655 hydrochloride inhibits AMPA receptor-mediated responses in cerebella Purkinje neurons with an IC50 value of 1.5±0.1 μM[1].
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. 143692-48-2
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Appearance Solid
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Molecular Weight 388.85
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Formula C19H21ClN4O3
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Color Light yellow to yellow
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SMILES
O=C(N1N=C(C2=CC=C(N)C=C2)C3=CC(OCO4)=C4C=C3CC1C)NC.[H]Cl
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Synonyms
LY300168 hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
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Nat Neurosci
Excitatory synapses onto axonic spines jump-start action potentials and route information flow. [Abstract]2026 May 15. PMID: 42141306
Solvent & Solubility
DMSO : ≥ 160 mg/mL (411.47 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 8 mg/mL (20.57 mM; Need ultrasonic and warming)
* "≥" means soluble, but saturation unknown.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocol
Whole-cell voltage clamp recordings are made from single cells with use of the tight seal whole cell configuration of the patch-clamp technique. Experiments are performed at room temperature (20 to 22°C) and recorded on an amplifier. GYKI 53655 hydrochloride application is via a series of perfusion lines to a multi-barrelled applicator and exchange of solutions under the present recording conditions is approximately 100 msec. For the acutely isolated cerebella Purkinje neurons, GYKI 53655 hydrochloride application is by bath perfusion and occurs within approximately 15 sec. Curve fitting to data points is based upon the equationy=100(Dn/(Dn+IC50n)), where the slope of the line n is fixed to a value of 1 and D is the antagonist concentration. Statistical significance is determined by one-way ANOVA followed by Student- Newman-Keulstest[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Experiments are performed on 27 male Wistar rats (260 to 350 g). Briefly, rats are anaesthetized with halothane in O2 and tracheal, carotid and jugular cannulae are inserted. The lumbo-thoracic spinal cord is exposed and cut at T9-T11 and the animal is prepared for extracellular recordings of single dorsal horn neurone action potentials. Anaesthesia after surgery is maintained with α-chloralose. Jugular cannulae are inserted. GYKI 53655 hydrochloride is administered intravenously. The effect of GYKI 53655 hydrochloride is expressed quantitatively as percentages of control excitatory amino acids (EAA) responses, where control is taken as the mean of the last 3 pre-drug counts; mean values±s.e.mean are indicated. No corrections for spontaneous activity are made[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (279 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]. Bleakman D, et al. Activity of 2,3-benzodiazepines at native rat and recombinant human glutamate receptors in vitro: stereospecificity and selectivity profiles. Neuropharmacology. 1996;35(12):1689-702. [Content Brief]
[2]. Chizh BA, et al. A comparison of intravenous NBQX and GYKI 53655 as AMPA antagonists in the rat spinal cord. Br J Pharmacol. 1994 Jul;112(3):843-6. [Content Brief]
[3]. Szabados T, et al. Comparison of anticonvulsive and acute neuroprotective activity of three 2,3-benzodiazepine compounds, GYKI 52466, GYKI 53405, and GYKI 53655. Brain Res Bull. 2001 Jun;55(3):387-91. [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 (sealed storage, away from moisture). 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 |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.5717 mL | 12.8584 mL | 25.7169 mL | 64.2921 mL |
| 5 mM | 0.5143 mL | 2.5717 mL | 5.1434 mL | 12.8584 mL | |
| 10 mM | 0.2572 mL | 1.2858 mL | 2.5717 mL | 6.4292 mL | |
| 15 mM | 0.1714 mL | 0.8572 mL | 1.7145 mL | 4.2861 mL | |
| 20 mM | 0.1286 mL | 0.6429 mL | 1.2858 mL | 3.2146 mL | |
| DMSO | 25 mM | 0.1029 mL | 0.5143 mL | 1.0287 mL | 2.5717 mL |
| 30 mM | 0.0857 mL | 0.4286 mL | 0.8572 mL | 2.1431 mL | |
| 40 mM | 0.0643 mL | 0.3215 mL | 0.6429 mL | 1.6073 mL | |
| 50 mM | 0.0514 mL | 0.2572 mL | 0.5143 mL | 1.2858 mL | |
| 60 mM | 0.0429 mL | 0.2143 mL | 0.4286 mL | 1.0715 mL | |
| 80 mM | 0.0321 mL | 0.1607 mL | 0.3215 mL | 0.8037 mL | |
| 100 mM | 0.0257 mL | 0.1286 mL | 0.2572 mL | 0.6429 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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