Zervimesine
Based on 1 publication(s) in Google Scholar
Zervimesine (CT1812) is an orally active and brain penetrant sigma-2 receptor antagonist with a Ki of 8.5 nM. Zervimesine can be used for the research of Alzheimer’s disease.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.01%
- CAS. Nr.: 1802632-22-9
- Formel: C24H33NO4S
- Molecular Weight:431.59
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Speicherung:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Biologische Aktivität
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Chemical Information
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- Reinheit & Dokumentation
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Publications Citing Use of MedChemExpress (MCE) Zervimesine
MoreAlle Sigma Receptor Isoform-spezifische Produkte anzeigen
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Biologische Aktivität
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Sigma 2 Receptor |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Neuron | EC50 |
358 μM
Compound: 7; CT1812
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Reversal of amyloid beta oligomer-induced vesicular membrane trafficking in Sprague-Dawley rat neurons pretreated with amyloid beta oligomer for 1 hr followed by compound treatment by ELISA
Reversal of amyloid beta oligomer-induced vesicular membrane trafficking in Sprague-Dawley rat neurons pretreated with amyloid beta oligomer for 1 hr followed by compound treatment by ELISA
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[PMID: 34531947] |
| Neuron | EC50 |
6.8 μM
Compound: 7; CT1812
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Prevention of vesicular membrane trafficking in Sprague-Dawley rat neurons assessed as inhibition of amyloid beta oligomer binding to nuclear receptor pretreated with compounds followed by amyloid beta oligomer challenge and measured after 1 hr by ELISA
Prevention of vesicular membrane trafficking in Sprague-Dawley rat neurons assessed as inhibition of amyloid beta oligomer binding to nuclear receptor pretreated with compounds followed by amyloid beta oligomer challenge and measured after 1 hr by ELISA
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[PMID: 34531947] |
Zervimesine (CT1812) (0.0001-10 μM, 30 min) displaces and prevents Aβ oligomer binding in neurons and glia[1].
Zervimesine (4.8 μM, 48 h) increases synaptic number and protein expression in neurons[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Zervimesine (10 mg/kg, p.o., daily, 9-10 weeks) improves cognitive performance in transgenic Thy1 huAPPSwe/Lnd+ male mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 1802632-22-9
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Appearance Solid
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Molecular Weight 431.59
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Formel C24H33NO4S
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Color White to off-white
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SMILES
OC1=CC=C(CCC(C)(N2CC3=C(C=C(S(=O)(C)=O)C=C3)C2)C)C=C1OC(C)(C)C
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Synonyms
CT1812; Sigma-2 receptor antagonist 1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (1)
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Journal Impact Factor
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Most Recent
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J Cell Mol Med
The Sigma-2 Receptor/TMEM97 Agonist PB28 Suppresses Cell Proliferation and Invasion by Regulating the PI3K-AKT-mTOR Signalling Pathway in Renal Cancer. [Abstract]2021 Dec;25(24):11244-11256. PMID: 34783163
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (231.70 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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: ≥ 2.08 mg/mL (4.82 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.82 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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.
Reinheit & Dokumentation
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Data Sheet (272 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)
Verweise
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 | 2.3170 mL | 11.5851 mL | 23.1701 mL | 57.9253 mL |
| 5 mM | 0.4634 mL | 2.3170 mL | 4.6340 mL | 11.5851 mL | |
| 10 mM | 0.2317 mL | 1.1585 mL | 2.3170 mL | 5.7925 mL | |
| 15 mM | 0.1545 mL | 0.7723 mL | 1.5447 mL | 3.8617 mL | |
| 20 mM | 0.1159 mL | 0.5793 mL | 1.1585 mL | 2.8963 mL | |
| 25 mM | 0.0927 mL | 0.4634 mL | 0.9268 mL | 2.3170 mL | |
| 30 mM | 0.0772 mL | 0.3862 mL | 0.7723 mL | 1.9308 mL | |
| 40 mM | 0.0579 mL | 0.2896 mL | 0.5793 mL | 1.4481 mL | |
| 50 mM | 0.0463 mL | 0.2317 mL | 0.4634 mL | 1.1585 mL | |
| 60 mM | 0.0386 mL | 0.1931 mL | 0.3862 mL | 0.9654 mL | |
| 80 mM | 0.0290 mL | 0.1448 mL | 0.2896 mL | 0.7241 mL | |
| 100 mM | 0.0232 mL | 0.1159 mL | 0.2317 mL | 0.5793 mL |
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