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| 1mg |
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| 5mg |
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| 10mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| ln Vitro |
The effects of ZSET1446 (100 pM–10 nM) on synaptic transmission and basal neuron excitability are minimal. ZSET1446 amplifies the nAChR stimulation's encouraging effect on sPSC frequency. ZSET1446 does not alter basal sIPSC frequency in the range of 10 pM to 1 nM, but it does improve the increase in sIPSC frequency by topical application of nicotine (5 µM; 2 minutes) [1].
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| ln Vivo |
ZSET1446 ameliorates scopolamine-induced cognitive impairment in rats and improves object recognition memory in mice. ZSET1446 and memantine administered at sub-effective levels concurrently considerably enhanced cognitive performance in novel object identification tasks in rats and mice. Moreover, compared to controls, oral treatment of ZSET1446 or memantine raised extracellular ACh levels in the hippocampal regions. Furthermore, compared to the ZSET1446 or memantine group alone, the coadministration of sub-effective dosages of ZSET1446 and memantine markedly raised extracellular ACh levels [2]. After 4, 8, 12, and 16 weeks of treatment, ZSET1446 (0.002, 0.01, and 0.1 mg/kg, orally) corrected SAMP8 cognitive deficiencies in a novel object recognition test. 16 weeks of treatment with ZSET1446 also resulted in lower SAMP8 grade points. Moreover, an 8-week treatment with ZSET1446 markedly decreased the overall quantity of Aβ-positive granules in the hippocampus [3].
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| References |
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| Additional Infomation |
ST-101 is a small peptide antagonist of C/EBPβ and T-type calcium channel activator. ST101 has been used in trials studying the treatment of Essential Tremor and Alzheimer's Disease.
Ismidenon is an orally bioavailable azaindolizinone derivative and acetylcholine releasing agent, with potential neurocognitive-enhancing activity. Upon oral administration, ismidenon increases acetylcholine release in the central nervous system (CNS), thereby enhancing cholinergic neurotransmission. Ismidenon also decreases amyloid beta peptide production. This may improve neurocognitive function in Alzheimer's disease. |
| Molecular Formula |
C15H12N2O
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|---|---|
| Molecular Weight |
236.27
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| Exact Mass |
236.095
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| CAS # |
887603-94-3
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| PubChem CID |
10220323
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| Appearance |
Light yellow to khaki solid powder
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| LogP |
0.858
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
18
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| Complexity |
475
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
QZWYXEBIQWJXAR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H12N2O/c18-14-15(17-8-4-3-7-13(17)16-14)9-11-5-1-2-6-12(11)10-15/h1-8H,9-10H2
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| Chemical Name |
spiro[1,3-dihydroindene-2,3'-imidazo[1,2-a]pyridine]-2'-one
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| Synonyms |
ZSET1446; ST-101; ZSET-1446
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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 : ~50 mg/mL (~211.62 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.58 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 (10.58 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 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (10.58 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 | 4.2324 mL | 21.1622 mL | 42.3245 mL | |
| 5 mM | 0.8465 mL | 4.2324 mL | 8.4649 mL | |
| 10 mM | 0.4232 mL | 2.1162 mL | 4.2324 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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