2. PI3K/Akt/mTOR Neuronal Signaling Membrane Transporter/Ion Channel
  3. mTOR iGluR Amyloid-β Tau Protein
  4. Simufilam

Simufilam (PTI-125) is an orally active FLNA modulator. Simufilam restores NMDAR signaling and Arc expression. Simufilam inhibits overactive mTOR signaling by restoring the normal conformation of FLNA, improves insulin sensitivity, reduces Aβ42-induced neuroinflammation and tau protein hyperphosphorylation. Simufilam can be used for research of Alzheimer's disease.

For research use only. We do not sell to patients.

Simufilam Chemical Structure

Simufilam Chemical Structure

CAS No. : 1224591-33-6

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

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Simufilam Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Simufilam

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AMPA Receptor NMDA Receptor Kainate Receptor

  • Biological Activity

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  • Customer Review

Description

Simufilam (PTI-125) is an orally active FLNA modulator. Simufilam restores NMDAR signaling and Arc expression. Simufilam inhibits overactive mTOR signaling by restoring the normal conformation of FLNA, improves insulin sensitivity, reduces Aβ42-induced neuroinflammation and tau protein hyperphosphorylation. Simufilam can be used for research of Alzheimer's disease[1][2][3].

In Vitro

Simufilam (1 nM; 1 h) reduces FLNA-α7nAChR/TLR4 associations, dissociates Aβ42-α7nAChR complexes, restores α7nAChR/NMDAR/IR function, and decreases tau phosphorylation in postmortem human AD brain slices[2].
Simufilam (1 pM-1 nM; 1 h) dose-dependently reduces FLNA-α7nAChR/TLR4 associations, Aβ42-α7nAChR complexes, tau phosphorylation, and tau nitration, while restoring NMDAR signaling and Arc expression in postmortem human AD hippocampal slices[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Simufilam Related Antibodies
In Vivo

Simufilam (10 mg/kg; i.p.; daily; 2 weeks) reduces FLNA-α7nAChR/TLR4 associations, tau phosphorylation, Aβ42 aggregates, and inflammatory cytokines, while restoring α7nAChR/NMDAR/IR function in ICV Aβ42-infused mice[2].
Simufilam (30 mg/kg/d; p.o.; 2 months) reduces FLNA-α7nAChR/TLR4 associations, tau phosphorylation, Aβ42 deposits, and NFTs, improves NMDAR/IR function and synaptic plasticity, and enhances spatial/working memory and nesting behavior in 3xTg AD mice[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

259.35

Formula

C15H21N3O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1N(CC2=CC=CC=C2)C3(CCN(C)CC3)NC1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (192.79 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 3.8558 mL 19.2790 mL 38.5579 mL
5 mM 0.7712 mL 3.8558 mL 7.7116 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)

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Purity & Documentation

Purity: 98.08%

SDS (392 KB)

COA (255 KB) LCMS (88 KB)

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. 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 3.8558 mL 19.2790 mL 38.5579 mL 96.3948 mL
5 mM 0.7712 mL 3.8558 mL 7.7116 mL 19.2790 mL
10 mM 0.3856 mL 1.9279 mL 3.8558 mL 9.6395 mL
15 mM 0.2571 mL 1.2853 mL 2.5705 mL 6.4263 mL
20 mM 0.1928 mL 0.9639 mL 1.9279 mL 4.8197 mL
25 mM 0.1542 mL 0.7712 mL 1.5423 mL 3.8558 mL
30 mM 0.1285 mL 0.6426 mL 1.2853 mL 3.2132 mL
40 mM 0.0964 mL 0.4820 mL 0.9639 mL 2.4099 mL
50 mM 0.0771 mL 0.3856 mL 0.7712 mL 1.9279 mL
60 mM 0.0643 mL 0.3213 mL 0.6426 mL 1.6066 mL
80 mM 0.0482 mL 0.2410 mL 0.4820 mL 1.2049 mL
100 mM 0.0386 mL 0.1928 mL 0.3856 mL 0.9639 mL
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Simufilam Related Classifications

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:

Simufilam1224591-33-6PTI-125PTI125PTI 125mTORiGluRAmyloid-βTau ProteinMammalian target of RapamycinIonotropic glutamate receptorsβ-amyloid peptideAβAbetaInhibitorinhibitorinhibit

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