2. PROTAC Neuronal Signaling Membrane Transporter/Ion Channel
  3. Molecular Glues Calcium Channel Amyloid-β Tau Protein
  4. REM127

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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REM127

REM127 Chemical Structure

CAS No. : 1417823-67-6

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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REM127 Related Antibodies

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Description

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[1][2].

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.

REM127 Related Antibodies
In Vivo

REM127 (administered orally; daily dosing) restores hippocampal long-term potentiation in tauP301S transgenic mice with an ED50 of 6 mg/kg, and exerts no effect on wild-type animals[2].
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.

Animal Model: transgenic APP London mutant V717I; non-transgenic wild-type controls[2]
Dosage: 6 mg/kg/day (LTP rescue); unspecified dose (EEG studies)
Administration: p.o.; daily; 7 and 14 days
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.
Animal Model: bigenic APP-Ln:PS1(A246E) transgenic[2]
Dosage: 20 mg/kg
Administration: p.o.; daily; 3 months
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.
Animal Model: APP-SAA knock-in[2]
Dosage: 25 mg/kg
Administration: p.o.; daily; 3 months
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.
Molecular Weight

419.37

Formula

C20H20Cl2N4S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

ClC1=C(CCN2CCN(C3=NC(C4=CC=C(Cl)C=C4)=NS3)CC2)C=CC=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3845 mL 11.9226 mL 23.8453 mL
5 mM 0.4769 mL 2.3845 mL 4.7691 mL
View the 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.

  • Protocol 1

    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.
  • Protocol 2

    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:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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
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. 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
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

REM1271417823-67-6REM 127REM-127Molecular GluesCalcium ChannelAmyloid-βTau ProteinCa2+ channelsCa channelsβ-amyloid peptideAβAbetaseptin filamentiPSC-derived glutamate-releasing neuronsseptin 6/7synaptic functioncytosolic calciumhuman neuroblastoma cellsprimary rat hippocampal neuronsAlzheimer’s diseasehyperphosphorylated tautauP301LInhibitorinhibitorinhibit

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