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Progranulin modulator-1 (Compound 60) is an orally active enhancer of progranulin (PGRN) secretion. Progranulin modulator-1 enhances the potency of BV-2 cell to increase PGRN levels, has inhibitory effect on hERG and Low cytotoxicity, the PGRN EC50 and hERG IC50 were 83 and 3100 nM, respectively[1]. | [in vivo]
Progranulin modulator-1 (Compound 60) (i.v.: 1 mg/kg, p.o.: 10 mg/kg) has good mouse PK profiles, with high bioavailability and half-life, oral availability up to 99% and shows Kpuu > 1, indicating very favorable enrichment of in brain at 8 h post dosing, achieve a progranulin modulating effect with a relatively low dosage of Progranulin modulator-1[1].
Pharmacokinetic Parameters for Progranulin Modulator-1 in Mouse[1]
| PO t1/2 (h) | IV t1/2 (h) | Cmax,u (nM) | Kpuu @ 8 h | F (%) | CL | Vdss | | 4.8 | 7.4 | 62 | 2.91 | 99 | 2.08 | 15.2 |
| [References]
[1] Peng X, et al. Discovery of oxazoline enhancers of cellular progranulin release. Bioorg Med Chem Lett. 2023 Jan 15;80:129048. DOI:10.1016/j.bmcl.2022.129048 |
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