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Progranulin modulator-1

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Catalog No. T87248Cas No. 2641013-11-6

Progranulin Modulator-1 (Compound 60) is an orally active compound that promotes progranulin (PGRN) secretion. It enhances the ability of BV-2 cells to elevate PGRN levels, exhibits low cytotoxicity, and possesses an inhibitory effect on hERG. The EC50 for PGRN is 83 nM, and the IC50 for hERG is 3100 nM [1].

Progranulin modulator-1

Progranulin modulator-1

😃Good
Catalog No. T87248Cas No. 2641013-11-6
Progranulin Modulator-1 (Compound 60) is an orally active compound that promotes progranulin (PGRN) secretion. It enhances the ability of BV-2 cells to elevate PGRN levels, exhibits low cytotoxicity, and possesses an inhibitory effect on hERG. The EC50 for PGRN is 83 nM, and the IC50 for hERG is 3100 nM [1].
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
10 mgInquiry10-14 weeks10-14 weeks
50 mgInquiry10-14 weeks10-14 weeks
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Product Introduction

Bioactivity
Description
Progranulin Modulator-1 (Compound 60) is an orally active compound that promotes progranulin (PGRN) secretion. It enhances the ability of BV-2 cells to elevate PGRN levels, exhibits low cytotoxicity, and possesses an inhibitory effect on hERG. The EC50 for PGRN is 83 nM, and the IC50 for hERG is 3100 nM [1].
In vitro
Progranulin modulator-1 (Compound 60) exhibits an efflux ratio (ER) value of less than 2, indicating it is not a substrate of MDR, and demonstrates high binding affinity to brain tissue along with exceptional metabolic stability [1].
In vivo
Progranulin modulator-1 (Compound 60) (i.v.: 1 mg/kg, p.o.: 10 mg/kg) demonstrates a favorable pharmacokinetic profile in mice, with high bioavailability and a long half-life. It achieves an oral bioavailability of up to 99% and displays a Kpuu greater than 1, indicating significant brain accumulation within 8 hours post-administration, allowing for regulatory activity at relatively low dosages of Progranulin modulator-1 [1].
Chemical Properties
Molecular Weight369.41
FormulaC21H21F2N3O
Cas No.2641013-11-6
SmilesFC1=CC=C([C@@H]2N(CCC=3C2=CC=CC3)C4=N[C@@H](CO4)[C@@]5(F)CNC5)C=C1
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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