2. Neuronal Signaling Stem Cell/Wnt
  3. γ-secretase
  4. PF-06648671

PF-06648671?is a novel, brain-penetrable, and orally active γ-secretase modulator (GSM). PF-06648671 reduces Aβ42 and Aβ40, with concomitant increases in Aβ37 and Aβ38 in vitro. PF-06648671 is used for the study of Alzheimer’s disease.

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

PF-06648671 Chemical Structure

PF-06648671 Chemical Structure

CAS No. : 1587727-31-8

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Based on 1 publication(s) in Google Scholar

PF-06648671 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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Description

PF-06648671?is a novel, brain-penetrable, and orally active γ-secretase modulator (GSM). PF-06648671 reduces Aβ42 and Aβ40, with concomitant increases in Aβ37 and Aβ38 in vitro. PF-06648671 is used for the study of Alzheimer’s disease[1].
IC50 & Target

IC50: γ-secretase[1]
Cellular Effect
Cell Line Type Value Description References
CHO EC50
8 nM
Compound: 80
Modulation of gamma-secretase in CHO cells expressing human APP assessed as reduction in amyloid beta (1 to 42 residues) production after 24 hrs by ELISA
Modulation of gamma-secretase in CHO cells expressing human APP assessed as reduction in amyloid beta (1 to 42 residues) production after 24 hrs by ELISA
[PMID: 27007185]
In Vitro

In a cell-based assay, PF-06648671 reduces Aβ42 and Aβ40 , with concomitant increases in Aβ37 and Aβ38, without inhibiting the cleavage of Notch or other substrates[1].

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

PF-06648671 Related Antibodies
In Vivo

PF-06648671 demonstrates reduces Aβ42 within the brain and CSF following acute oral administration in animals[1].

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

538.92

Formula

C25H23ClF4N4O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

FC(F)(C(C=C1Cl)=C([C@](CC2)([H])O[C@]2([H])[C@@H](N(CCN3C4=CC=C(N5C=NC(C)=C5)C3=O)C4=O)C)C=C1F)F
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 : 125 mg/mL (231.95 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 1.8556 mL 9.2778 mL 18.5556 mL
5 mM 0.3711 mL 1.8556 mL 3.7111 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.

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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: ≥ 2.08 mg/mL (3.86 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (3.86 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

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

Purity: 98.12%

SDS (251 KB)

COA (249 KB) LCMS (89 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 1.8556 mL 9.2778 mL 18.5556 mL 46.3891 mL
5 mM 0.3711 mL 1.8556 mL 3.7111 mL 9.2778 mL
10 mM 0.1856 mL 0.9278 mL 1.8556 mL 4.6389 mL
15 mM 0.1237 mL 0.6185 mL 1.2370 mL 3.0926 mL
20 mM 0.0928 mL 0.4639 mL 0.9278 mL 2.3195 mL
25 mM 0.0742 mL 0.3711 mL 0.7422 mL 1.8556 mL
30 mM 0.0619 mL 0.3093 mL 0.6185 mL 1.5463 mL
40 mM 0.0464 mL 0.2319 mL 0.4639 mL 1.1597 mL
50 mM 0.0371 mL 0.1856 mL 0.3711 mL 0.9278 mL
60 mM 0.0309 mL 0.1546 mL 0.3093 mL 0.7732 mL
80 mM 0.0232 mL 0.1160 mL 0.2319 mL 0.5799 mL
100 mM 0.0186 mL 0.0928 mL 0.1856 mL 0.4639 mL
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PF-06648671 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:

PF-066486711587727-31-8PF06648671PF 06648671γ-secretaseGamma secretaseInhibitorinhibitorinhibit

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