| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| Other Sizes |
|
| 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].
|
|---|---|
| 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].
|
| References |
|
| Molecular Formula |
C14H17F3N3O7P
|
|---|---|
| Molecular Weight |
427.269654989243
|
| Exact Mass |
427.075
|
| CAS # |
1255517-78-2
|
| Related CAS # |
Fanapanel;161605-73-8
|
| PubChem CID |
71312017
|
| Appearance |
Light yellow to yellow solid powder
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
11
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
28
|
| Complexity |
651
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
RYQLMFHPDNKPKY-UHFFFAOYSA-N
|
| 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
|
| Chemical Name |
[7-morpholin-4-yl-2,3-dioxo-6-(trifluoromethyl)-4H-quinoxalin-1-yl]methylphosphonic acid;hydrate
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~5 mg/mL (~11.70 mM)
H2O : ~5 mg/mL (~11.70 mM) |
|---|---|
| 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
