Progranulin modulator-1 

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].

EC50: 83 nM (PGRN); IC50: 3100 nM (hERG)

Progranulin modulator-1 (Compound 60) has an efflux ratio (ER) value <2, indicating that it is not a substrate for MDR and shows high brain tissue binding and high metabolic stability^[1].
Progranulin modulator-1 In vitro ADME properties for selected molecules^[1]

Progranulin modulator-1的体外ADME特性^[1]

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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 K_puu > 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]

小鼠体内Progranulin Modulator-1 的药代动力学参数^[1]

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

369.41

C₂₁H₂₁F₂N₃O

2641013-11-6

FC1=CC=C(C=C1)[C@@H]2N(C3=N[C@H](C4(CNC4)F)CO3)CCC5=CC=CC=C52

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Peng X, et al. Discovery of oxazoline enhancers of cellular progranulin release. Bioorg Med Chem Lett. 2023 Jan 15;80:129048.  [Content Brief]