| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Targets |
ZK-200775 targets the AMPA (α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid) and kainate receptors, which are subtypes of ionotropic glutamate receptors. It acts as a highly selective competitive antagonist with little activity against NMDA receptors. It has Ki values of 3.2 nM for the AMPA receptor (quisqualate site) and 100 nM for the kainate receptor. Its high affinity for AMPA receptors underlies its neuroprotective effects.
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| ln Vitro |
ZK200775 demonstrated Ki values of 3.2 nM, 100 nM, and 8.5 μM for cisternate, kainic acid, and NMDA in cortical slice preparation experiments, respectively. Its IC50 values in experiments for diffusion inhibition are 200 nM, 76 nM, 13 μM, and 18 μM for quilacine, kainic acid, NMDA, and glycine [1].
In vitro, ZK-200775 is a highly potent and selective AMPA/kainate receptor antagonist. In cortical slice preparation assays, it demonstrates Ki values of 3.2 nM against quisqualate (AMPA), 100 nM against kainate, and 8.5 µM against NMDA. This indicates a high degree of selectivity for AMPA receptors over NMDA receptors. Its activity is typically assessed using electrophysiological techniques or radioligand binding assays. |
| ln Vivo |
ZK200775 increases the threshold for clonic seizures induced by AMPA and kainic acid in mice, with THRD50 (threshold dose) of 2.9 (1.7-4.6) and 1.6 (1.3-2.0) mg/kg iv, whereas NMDA-induced epilepsy The seizure threshold was dose-only elevated, THRD50 24.1 (21.9–26.5) mg/kg iv, affecting motor coordination of the rotarod, ED50 14.6 (12.1–17.6) mg/kg. Intravenous dosages of ZK200775 at 10 and 30 mg/kg lowered muscular tone in rats with hereditary spasticity [1]. ZK200775 (3.0, but not 1.5 or 6.0 mg/kg) significantly reduced nicotine-induced (0.6 mg/kg) DA release in NAcc and nicotine-stimulated LMA. ZK200775 (1.5, 3.0, 6.0 mg/kg) alone impacted neither DA release nor LMA. ZK200775 is 34 times more selective for AMPA receptors than NMDA receptors and has no affinity for nicotine receptors
In vivo, ZK-200775 has demonstrated neuroprotective efficacy in experimental models of stroke. It has also been shown to inhibit nicotine-induced dopamine release in the nucleus accumbens. It has been evaluated for tolerability in healthy volunteers. These findings support its potential for the treatment of neurological conditions involving excitotoxicity. |
| Enzyme Assay |
The in vitro receptor binding assay for ZK-200775 typically involves radioligand displacement studies using membrane preparations from brain tissue or cells expressing AMPA and kainate receptors. The compound's affinity (Ki) is determined by measuring its ability to displace a specific radiolabeled ligand, such as [3H]AMPA or [3H]kainate, from these receptors. Its selectivity is assessed by testing against NMDA receptors.
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| Cell Assay |
In vitro cellular assays for ZK-200775 assess its functional antagonism at AMPA receptors. This typically involves electrophysiological recordings from neurons or cells expressing AMPA receptors to measure the inhibition of glutamate- or quisqualate-induced currents. Calcium imaging assays can also be used to measure the compound's ability to block AMPA receptor-mediated calcium influx. These assays confirm its functional antagonistic activity.
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| Animal Protocol |
In vivo animal studies for ZK-200775 have been conducted in experimental models of stroke to evaluate its neuroprotective efficacy. It has also been studied in models of addiction to assess its effects on dopamine release. The compound is typically administered systemically, and endpoints such as infarct volume or behavioral changes are measured.
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| ADME/Pharmacokinetics |
Specific pharmacokinetic data for ZK-200775 are not extensively detailed in the available literature. As a small molecule, its pharmacokinetic properties would be important for its in vivo efficacy. However, specific parameters such as half-life and bioavailability are not provided. It has been evaluated in healthy volunteers, indicating it has suitable pharmacokinetic properties for human use.
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| Toxicity/Toxicokinetics |
Specific toxicity data for ZK-200775 are not extensively detailed in the available literature. However, possible glial cell toxicity has been detected by monitoring S-100B serum levels. Its tolerability in healthy volunteers has been demonstrated. Comprehensive toxicological studies would be required for clinical development. It is intended for research purposes only.
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| References |
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| Additional Infomation |
Fanapanel has been studied for its potential use in treating visual impairment.
ZK-200775 (Fanapanel) is a highly selective competitive AMPA/kainate receptor antagonist with Ki values of 3.2 nM, 100 nM, and 8.5 µM against quisqualate, kainate, and NMDA, respectively. It has demonstrated neuroprotective efficacy in stroke models. It is a research compound for studying excitotoxicity and neurological disorders. It is not approved for clinical use. |
| Molecular Formula |
C14H15N3O6F3P
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|---|---|
| Molecular Weight |
409.2544
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| Exact Mass |
409.065
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| CAS # |
161605-73-8
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| Related CAS # |
Fanapanel hydrate;1255517-78-2
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| PubChem CID |
208953
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| Appearance |
White to off-white solid powder
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| Density |
1.6±0.1 g/cm3
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| Index of Refraction |
1.564
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| LogP |
-0.55
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
27
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| Complexity |
651
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
WZMQMKNCWDCCMT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H15F3N3O6P/c15-14(16,17)8-5-9-11(6-10(8)19-1-3-26-4-2-19)20(7-27(23,24)25)13(22)12(21)18-9/h5-6H,1-4,7H2,(H,18,21)(H2,23,24,25)
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| Chemical Name |
[7-morpholin-4-yl-2,3-dioxo-6-(trifluoromethyl)-4H-quinoxalin-1-yl]methylphosphonic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~1.25 mg/mL (~3.05 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4435 mL | 12.2175 mL | 24.4349 mL | |
| 5 mM | 0.4887 mL | 2.4435 mL | 4.8870 mL | |
| 10 mM | 0.2443 mL | 1.2217 mL | 2.4435 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00999284 | Completed | Drug: ZK200775 Drug: ZK200775 Drug: Sodium Chloride |
Visual Acuity | Charite University, Berlin, Germany | 1996-12 | Phase 1 |
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