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Pack Size | Price | Availability | Quantity |
---|---|---|---|
10 mg | Inquiry | 10-14 weeks | |
50 mg | Inquiry | 10-14 weeks |
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 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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