Art. -Nr.: HY-120789

PF-06648671

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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.

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Reinheit: 99.25%
CAS. Nr.: 1587727-31-8
Formel: C₂₅H₂₃ClF₄N₄O₃
Molecular Weight:538.92

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

PF-06648671 Chemical Structure

CAS. Nr.: 1587727-31-8

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

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.

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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1587727-31-8
Appearance Solid
Molecular Weight 538.92
Formel C₂₅H₂₃ClF₄N₄O₃
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.8556 mL

9.2778 mL

18.5556 mL

5 mM

0.3711 mL

1.8556 mL

3.7111 mL

10 mM

0.1856 mL

0.9278 mL

1.8556 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Jae Eun Ahn, et al. Pharmacokinetic and Pharmacodynamic Effects of a γ-Secretase Modulator, PF-06648671, on CSF Amyloid-β Peptides in Randomized Phase I Studies. Clin Pharmacol Ther 2020 Jan;107(1):211-220. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

MCE Bioactive Compound Library

Clinical Compound Library Plus

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

PF-06648671

MCE Bioactive Compound Library

Clinical Compound Library Plus

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

PF-06648671 Related Classifications

HY-120789 Related Classifications