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Zonampanel (YM-872) is a novel and potent AMPA receptor antagonist with the potential to be used for the treatment of stroke.
| ln Vitro |
In a concentration-dependent manner, zonampanel blocks the human MRP4-mediated transport of [3H]oestradiol 17-D-glucuronide. However, the human MRP2- or BCRP-mediated transport of [3H]oestradiol 17-D-glucuronide or [3H]methotrexate is not inhibited by zonampanel (up to 1000 mM)[1]. For Oat1, Oat2, and Oat3, zonampanel reduces the absorption of typical substrates with inhibition constants (Ki) ranging from 7.02 to 10.4 μM. These cells exhibit a time- and concentration-dependent increase in [14C]Zonampanel uptake [Km values: 13.4 to 53.6 μM].[2].
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| ln Vivo |
Probenecid and cimetidine have been shown in in vivo studies to reduce intrinsic clearance for Zonampanel's biliary excretion as well as renal secretion[2].
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| References |
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| Molecular Formula |
C13H9N5O6
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|---|---|
| Molecular Weight |
331.244
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| Exact Mass |
331.055
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| CAS # |
210245-80-0
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| PubChem CID |
148200
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| Appearance |
Yellow to brown solid powder
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| LogP |
0.391
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
24
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| Complexity |
578
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
SPXYHZRWPRQLNS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H9N5O6/c19-11(20)5-17-8-4-9(16-2-1-14-6-16)10(18(23)24)3-7(8)15-12(21)13(17)22/h1-4,6H,5H2,(H,15,21)(H,19,20)
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| Chemical Name |
2-(7-imidazol-1-yl-6-nitro-2,3-dioxo-4H-quinoxalin-1-yl)acetic acid
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| Synonyms |
YM872 YM-872 Zonampanel
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 : ~50 mg/mL (~150.95 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.55 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 25.0 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: 2.5 mg/mL (7.55 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0190 mL | 15.0948 mL | 30.1896 mL | |
| 5 mM | 0.6038 mL | 3.0190 mL | 6.0379 mL | |
| 10 mM | 0.3019 mL | 1.5095 mL | 3.0190 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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