Size : 10mg
Synonyms:
| 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]. |
| Molecular Weight | 369.41 |
| Formula | C21H21F2N3O |
| Cas No. | 2641013-11-6 |
| Smiles | FC1=CC=C([C@@H]2N(CCC=3C2=CC=CC3)C4=N[C@@H](CO4)[C@@]5(F)CNC5)C=C1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Dissolve 2 mg of the compound in 100 μL DMSO 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.
1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 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 ddH2O and mix thoroughly until a homogeneous solution is obtained.
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