REM127
Based on 1 Customer Validation
REM127 is an orally active, blood-brain barrier-penetrant septin 6/7 molecular glue degrader. REM127 binds to SEPT6 with high affinity and promotes the assembly of SEPT2/6/7 cortical filaments, thereby normalizing cytoplasmic calcium levels, cerebrospinal fluid hyperphosphorylated tau protein levels, synaptic function and cognitive function. REM127 can be used in research related to Alzheimer's disease.
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- Pureté: 99.46%
- CAS No.: 1417823-67-6
- Formule: C20H20Cl2N4S
- Masse moléculaire:419.37
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Stockage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
In Vitro
REM127 restores calcium homeostasis, improves synaptic function, reduces Alzheimer's disease-related tau and Aβ pathology, and rescues survival of neuronal cells challenged with pathological tau or Aβ[1].
REM127 (15-19 nM) potently reduces tauP301L-induced toxicity and restores calcium homeostasis in neuronally differentiated human neuroblastoma cells with EC50 values of 15 nM and 19 nM, respectively[2].
REM127 restores dendritic spine density and rescues primary rat hippocampal neurons from ADDL-induced cell death[2].
REM127 selectively normalizes tauP301L-induced aberrant SOCE and elevated basal cytoplasmic calcium levels in human neuroblastoma cells without affecting physiological calcium signaling in control cells[2].
REM127 selectively normalizes elevated SOCE in patient iPSC-derived tauP301L-expressing glutamate-releasing neurons without affecting physiological SOCE in isogenic control neurons[2].
REM127 reduces tauP301L-induced increases in ER-PM contact area in human neuroblastoma cells[2].
REM127 normalizes calcium2+-dependent NFAT signaling by inhibiting tauP301L-induced NFAT nuclear translocation in human neuroblastoma cells[2].
REM127 restores cortical septin filament organization disrupted by tauP301L expression in human neuroblastoma cells[2].
REM127 fully rescues hyperexcitability in patient iPSC-derived tauP301L-expressing glutamate-releasing neurons over 20 days of treatment[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
REM127 (20 mg/kg; p.o.; once daily; for 7-14 consecutive days) restores hippocampal long-term potentiation in APP-Ln transgenic mice, and normalizes brain oscillatory activity after 14 days of administration[2].
REM127 (20 mg/kg; p.o.; once daily; for 3 months) reduces Aβ plaque burden and microglial inflammation levels in double-transgenic mice[2].
REM127 (25 mg/kg; p.o.; once daily; for 3 months) reduces dense-core amyloid plaques, Aβ42 production, and phosphorylated tau protein aggregation in APP-SAA knock-in mice[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:transgenic APP London mutant V717I; non-transgenic wild-type controls[2]
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Dosage:6 mg/kg/day (LTP rescue); unspecified dose (EEG studies)
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Administration:p.o.; daily; 7 and 14 days
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Result:Restored hippocampal LTP in APP-Ln mice with severe LTP deficits in untreated state; a 7-day treatment was sufficient for LTP rescue.
Normalized the elevated low-frequency theta rhythm power spectral density seen in untreated APP-Ln mice after 14 days of treatment.
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Animal Model:bigenic APP-Ln:PS1(A246E) transgenic[2]
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Dosage:20 mg/kg
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Administration:p.o.; daily; 3 months
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Result:Reduced neocortical Aβ plaque buildup by 55 to 60% and subicular Aβ plaque buildup by 55 to 60%.
Reduced microglial inflammation associated with AD pathology.
Lowered both total and dense-core plaque load.
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Animal Model:APP-SAA knock-in[2]
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Dosage:25 mg/kg
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Administration:p.o.; daily; 3 months
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Result:Decreased dense-core amyloid plaques and Aβ42 production in the prefrontal cortex.
Markedly reduced AT8 immunoreactivity (a marker of phosphorylated tau aggregates) in the prefrontal cortex.
Chemical Information
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CAS No. 1417823-67-6
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Appearance Solid
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Masse moléculaire 419.37
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Formule C20H20Cl2N4S
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Color White to off-white
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SMILES
ClC1=C(CCN2CCN(C3=NC(C4=CC=C(Cl)C=C4)=NS3)CC2)C=CC=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 50 mg/mL (119.23 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. 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. 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: ≥ 1.25 mg/mL (2.98 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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: 1.25 mg/mL (2.98 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 1.25 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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.
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.
Pureté et documentation
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Fiche technique (276 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Nuytten M, et al. Randomized phase 2a trial assessing a novel septin molecular glue in Alzheimer's disease. Alzheimers Dement. 2025;21(9):e70537. [Content Brief]
[2]. Princen K, et al. Pharmacological modulation of septins restores calcium homeostasis and is neuroprotective in models of Alzheimer's disease. Science. 2024;384(6699):eadd6260. [Content Brief]
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. 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 | 2.3845 mL | 11.9226 mL | 23.8453 mL | 59.6132 mL |
| 5 mM | 0.4769 mL | 2.3845 mL | 4.7691 mL | 11.9226 mL | |
| 10 mM | 0.2385 mL | 1.1923 mL | 2.3845 mL | 5.9613 mL | |
| 15 mM | 0.1590 mL | 0.7948 mL | 1.5897 mL | 3.9742 mL | |
| 20 mM | 0.1192 mL | 0.5961 mL | 1.1923 mL | 2.9807 mL | |
| 25 mM | 0.0954 mL | 0.4769 mL | 0.9538 mL | 2.3845 mL | |
| 30 mM | 0.0795 mL | 0.3974 mL | 0.7948 mL | 1.9871 mL | |
| 40 mM | 0.0596 mL | 0.2981 mL | 0.5961 mL | 1.4903 mL | |
| 50 mM | 0.0477 mL | 0.2385 mL | 0.4769 mL | 1.1923 mL | |
| 60 mM | 0.0397 mL | 0.1987 mL | 0.3974 mL | 0.9936 mL | |
| 80 mM | 0.0298 mL | 0.1490 mL | 0.2981 mL | 0.7452 mL | |
| 100 mM | 0.0238 mL | 0.1192 mL | 0.2385 mL | 0.5961 mL |
REM127 Related Classifications
HY-162566 Related Classifications
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Keywords
- REM127
- 1417823-67-6
- REM 127
- REM-127
- Molecular Glues
- Calcium Channel
- Amyloid-β
- Tau Protein
- septin filament
- iPSC-derived glutamate-releasing neurons
- septin 6/7
- synaptic function
- cytosolic calcium
- human neuroblastoma cells
- primary rat hippocampal neurons
- Alzheimer’s disease
- hyperphosphorylated tau
- tauP301L
- Inhibitor
- inhibitor
- inhibit