uPSEM792
Based on 1 Customer Validation
uPSEM792 is a PSEM agonist of PSAM4-GlyR with blood-brain barrier permeability, activating PSAM4-GlyR to silence neuronal activity. uPSEM792 produces dose-dependent neuronal silencing effects in ex vivo retinal preparations, inhibiting calcium signaling responses in COMS‑AC amacrine cells. uPSEM792 flattens interstitial ion waves in hippocampal neurons expressing PSAM-GlyR and impairs cerebrospinal fluid perfusion and molecular clearance. uPSEM792 can be used for research on nervous system-related diseases.
For research use only. We do not sell to patients.
- Purity : 98.02%
- CAS No.: 2323525-19-3
- Formula: C14H15N3O
- Molecular Weight:241.29
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
In Vitro
uPSEM792 (10 nM) silences COMS-ACs via PSAM4-GlyR, reducing local inhibition of HD2p-RGCs and converting them from OMS-insensitive to OMS-sensitive[1].
uPSEM792 is an ultrapotent PSAM4‑GlyR chemogenetic agonist, with a Ki of 0.7 nM for PSAM4‑GlyR and Ki values of 8000 nM and 5.3 nM for α7‑nAChR and α4β2‑nAChR, respectively[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
uPSEM792 (3 mg/kg; i.p.; single acute injection during the efflux phase)-mediated silencing of efflux-phase neurons impairs molecular clearance and increases hippocampal tracer retention[2].
uPSEM792 (3 mg/kg; i.p.; single acute injection 1-1.5 h before cisterna magna contrast agent infusion)-mediated hippocampal silencing disrupts ipsilateral cerebrospinal fluid-to-parenchyma perfusion, whereas perivascular flow remains largely intact[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (adult 2-6 months)[2]
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Dosage:3 mg/kg
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Administration:i.p.; single acute injection
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Result:Reduced hippocampal neuronal action potentials to near‑undetectable levels and suppressed 0.5‑55 Hz power of anaesthetic‑state interstitial fluid ionic waves.
Impeded ipsilateral hippocampal CSF tracer infiltration; contralateral hippocampus and other brain regions remained unaltered, alongside stable frontal‑parietal EEG.
Flattened hippocampal interstitial fluid ionic waves across wake, NREM and REM states, with preserved cortical EEG activity.
Attenuated hippocampal CSF tracer perfusion in wakefulness and sleep, and generated greater inter‑hemispheric perfusion asymmetry during sleep.
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Animal Model:C57BL/6 (adult 2-6 months)[2]
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Dosage:3 mg/kg
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Administration:i.p.; single acute injection during efflux phase
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Result:Showed greater dextran‑Texas Red retention within the hippocampus throughout the efflux phase.
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Animal Model:C57BL/6 (adult 2-6 months)[2]
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Dosage:3 mg/kg
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Administration:i.p.; single acute injection 1-1.5 h before intracisterna magna contrast infusion
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Result:Disrupted ipsilateral CSF‑to‑parenchyma Dotarem perfusion via chemogenetic inhibition, leaving the contralateral hemisphere unimpaired.
Chemical Information
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CAS No. 2323525-19-3
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Appearance Solid
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Molecular Weight 241.29
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Formula C14H15N3O
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Color Off-white to light yellow
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SMILES
CN1C2=C(C=C(C3CNCC4C3)C4=C2)N=CC1=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
In Vitro:
DMSO : ≥ 100 mg/mL (414.44 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 9.5 mg/mL (39.37 mM); Clear solution
This protocol yields a clear solution of ≥ 9.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (95.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 9.5 mg/mL (39.37 mM); Clear solution
This protocol yields a clear solution of ≥ 9.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (95.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (280 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 4.1444 mL | 20.7220 mL | 41.4439 mL | 103.6098 mL |
| 5 mM | 0.8289 mL | 4.1444 mL | 8.2888 mL | 20.7220 mL | |
| 10 mM | 0.4144 mL | 2.0722 mL | 4.1444 mL | 10.3610 mL | |
| 15 mM | 0.2763 mL | 1.3815 mL | 2.7629 mL | 6.9073 mL | |
| 20 mM | 0.2072 mL | 1.0361 mL | 2.0722 mL | 5.1805 mL | |
| 25 mM | 0.1658 mL | 0.8289 mL | 1.6578 mL | 4.1444 mL | |
| 30 mM | 0.1381 mL | 0.6907 mL | 1.3815 mL | 3.4537 mL | |
| 40 mM | 0.1036 mL | 0.5180 mL | 1.0361 mL | 2.5902 mL | |
| 50 mM | 0.0829 mL | 0.4144 mL | 0.8289 mL | 2.0722 mL | |
| 60 mM | 0.0691 mL | 0.3454 mL | 0.6907 mL | 1.7268 mL | |
| 80 mM | 0.0518 mL | 0.2590 mL | 0.5180 mL | 1.2951 mL | |
| 100 mM | 0.0414 mL | 0.2072 mL | 0.4144 mL | 1.0361 mL |
uPSEM792 Related Classifications
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