| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Fanapanel targets AMPA (alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid) receptors and kainate receptors, which are ionotropic glutamate receptors that mediate fast excitatory neurotransmission in the central nervous system. The compound has Ki values of 3.2 nM against quisqualate (AMPA receptor), 100 nM against kainate, and 8.5 microM against NMDA. This demonstrates high selectivity for AMPA receptors over NMDA receptors. By blocking AMPA and kainate receptors, fanapanel inhibits glutamate-mediated excitatory neurotransmission. The compound's high selectivity for AMPA/kainate over NMDA makes it a valuable tool for studying the specific roles of AMPA and kainate receptors in synaptic transmission, plasticity, and excitotoxicity.
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| ln Vitro |
In cortical slice preparation experiments, ZK200775 had Ki values of 3.2 nM, 100 nM, and 8.5 μM for cisternate, kainic acid, and NMDA, respectively. In diffusion inhibition experiments, it possesses IC50 values of 200 nM, 76 nM, 13 μM and 18 μM against quilacine, kainic acid, NMDA and glycine [1].
Fanapanel hydrate demonstrates potent in vitro activity as an AMPA/kainate receptor antagonist. The compound has Ki values of 3.2 nM against quisqualate (AMPA receptor), 100 nM against kainate, and 8.5 microM against NMDA. This demonstrates high potency and selectivity for AMPA receptors. The compound is a highly selective AMPA antagonist. Its activity is concentration-dependent, with potent inhibition observed at nanomolar concentrations. Fanapanel hydrate is used in neuroscience research to study AMPA receptor function and excitatory neurotransmission. Its selectivity for AMPA/kainate over NMDA makes it a valuable tool for dissecting the roles of different glutamate receptor subtypes. |
| ln Vivo |
ZK200775 raises the threshold for clonic seizures in mice induced by AMPA and kainic acid, with THRD50 (threshold dose) of 2.9 (1.7-4.6) and 1.6 (1.3-2.0) mg/kg iv. In contrast, the seizure threshold for NMDA-induced epilepsy was dose-only elevated, at THRD50 24.1 (21.9–26.5) mg/kg iv. This affected the rotarod's motor coordination, with an ED50 of 14.6 (12.1–17.6) mg/kg. In rats with hereditary spasticity, intravenous dosages of ZK200775 at 10 and 30 mg/kg decreased muscular tone [1]. In NAcc and nicotine-stimulated LMA, ZK200775 (3.0 mg/kg) significantly decreased nicotine-induced (0.6 mg/kg) DA release, but not 1.5 or 6.0 mg/kg. ZK200775 (1.5, 3.0, and 6.0 mg/kg) did not influence LMA or DA release on its own. ZK200775 shows little affinity for nicotine receptors and is 34 times more selective for AMPA receptors than NMDA receptors [2].
In vivo, fanapanel hydrate has been studied for its potential in conditions involving excessive glutamatergic neurotransmission, such as stroke, epilepsy, and neurodegenerative diseases. As an AMPA/kainate receptor antagonist, the compound inhibits excitatory neurotransmission and has potential neuroprotective effects. The compound's high selectivity for AMPA receptors makes it a valuable tool for studying the role of AMPA receptors in various neurological conditions. Comprehensive in vivo efficacy data have been reported in research publications. The compound's ability to cross the blood-brain barrier is relevant for its central nervous system effects. |
| Enzyme Assay |
In vitro receptor binding assays for fanapanel hydrate involve measuring binding affinity to AMPA and kainate receptors. Membranes from brain tissue or cells expressing AMPA or kainate receptors are incubated with radiolabeled ligands (e.g., [3H]-AMPA for AMPA receptors, [3H]-kainate for kainate receptors) and varying concentrations of the test compound. Bound and free radioligand are separated by filtration, and radioactivity is measured. Binding affinity (Ki) is calculated from competition curves using non-linear regression analysis. The compound has Ki values of 3.2 nM for quisqualate, 100 nM for kainate, and 8.5 microM for NMDA. Functional assays can measure inhibition of AMPA receptor-mediated currents using electrophysiological techniques. Each concentration is typically tested in duplicate or triplicate.
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| Cell Assay |
In vitro cellular assays for fanapanel hydrate are performed using neuronal cultures or cells expressing AMPA receptors. Cells are treated with AMPA or kainate to activate the receptors, and calcium influx or electrophysiological responses are measured. Varying concentrations of the test compound are added to assess inhibition of receptor-mediated responses. Calcium influx is measured using fluorescent calcium indicators such as Fluo-4 or Fura-2. Alternatively, electrophysiological recordings can be performed using patch-clamp techniques. Cytotoxicity is assessed in parallel using standard viability assays to ensure that observed effects are not due to cell death. IC50 values for inhibition of AMPA receptor-mediated responses are calculated from dose-response curves. The compound's selectivity for AMPA over NMDA is confirmed by comparing effects on AMPA and NMDA responses.
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| Animal Protocol |
In vivo animal studies for fanapanel hydrate are conducted using rodent models of stroke, epilepsy, and neurodegenerative diseases. The compound is administered via intraperitoneal injection, intravenous injection, or intracerebroventricular injection at various doses and schedules. In stroke models, infarct volume and neurological deficits are assessed. In epilepsy models, seizure activity is monitored. In neurodegenerative disease models, neuroprotection is assessed by measuring neuronal survival and behavioral outcomes. Pharmacokinetic studies assess drug concentrations in plasma and brain tissue. Animals are monitored for clinical signs and body weight. Efficacy is expressed as improvement in pathological or behavioral parameters compared to vehicle-treated controls.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of fanapanel hydrate have been characterized in preclinical studies. The compound has a molecular formula of C14H17F3N3O7P and a molecular weight of 427.27 g/mol. It is soluble in DMSO and other organic solvents. Comprehensive pharmacokinetic parameters including half-life, volume of distribution, clearance, and bioavailability have been characterized in animal models. The compound's ability to cross the blood-brain barrier is relevant for its central nervous system effects. Its pharmacokinetic profile supports its use in preclinical studies of neurological disorders. Detailed pharmacokinetic data are available from research publications.
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| Toxicity/Toxicokinetics |
Fanapanel hydrate is intended for laboratory research use only and has not undergone comprehensive clinical toxicology testing. As an AMPA/kainate receptor antagonist, the compound would be expected to have effects on neurotransmission and synaptic plasticity. Standard in vitro cytotoxicity assays in cell lines are typically performed alongside efficacy studies to rule out nonspecific toxicity. In vivo, animals are monitored for signs of toxicity including body weight changes, behavioral abnormalities, and clinical observations. Comprehensive toxicological characterization including genotoxicity and repeated-dose toxicity studies has been conducted as part of preclinical development. The compound is not approved for human use and is strictly intended for research purposes.
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| References |
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| Additional Infomation |
Fanapanel hydrate (ZK200775 hydrate, MPQX hydrate) is a highly selective AMPA/kainate receptor antagonist with Ki values of 3.2 nM for quisqualate, 100 nM for kainate, and 8.5 microM for NMDA. It has a molecular formula of C14H17F3N3O7P and a molecular weight of 427.27 g/mol. Fanapanel hydrate is used in neuroscience research to study AMPA receptor function and excitatory neurotransmission. The compound has not entered clinical trials and is available for research purposes only. Fanapanel hydrate is a valuable research tool for studying AMPA receptor pharmacology and developing new therapies for neurological disorders.
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| Molecular Formula |
C14H17F3N3O7P
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|---|---|
| Molecular Weight |
427.269654989243
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| Exact Mass |
427.075
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| CAS # |
1255517-78-2
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| Related CAS # |
Fanapanel;161605-73-8
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| PubChem CID |
71312017
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| Appearance |
Light yellow to yellow solid powder
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
28
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| Complexity |
651
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1COCCN1C2=CC3=C(C=C2C(F)(F)F)NC(=O)C(=O)N3CP(=O)(O)O.O
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| InChi Key |
RYQLMFHPDNKPKY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H15F3N3O6P.H2O/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);1H2
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| Chemical Name |
[7-morpholin-4-yl-2,3-dioxo-6-(trifluoromethyl)-4H-quinoxalin-1-yl]methylphosphonic acid;hydrate
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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 : ~5 mg/mL (~11.70 mM)
H2O : ~5 mg/mL (~11.70 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.5 mg/mL (1.17 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 5.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 0.5 mg/mL (1.17 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 5.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 0.5 mg/mL (1.17 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3404 mL | 11.7022 mL | 23.4044 mL | |
| 5 mM | 0.4681 mL | 2.3404 mL | 4.6809 mL | |
| 10 mM | 0.2340 mL | 1.1702 mL | 2.3404 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.
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