PK profiling was outsourced and undertaken by Shanghai ChemPartner Co., Ltd. All animal experiments performed were conducted in compliance with the Institutional Animal Care and Use Committee (IACUC) and the Office of Laboratory Animal Welfare (OLAW) guidelines. Six-to eight-week-old C57BL/6 male mice purchased from Jihui Laboratory Animal Co. LTD were used in the study. XL01126 was formulated in 10%HP-β-CD in 50mM Citrate buffer pH=3.0 at 1 mg/ml for IV injection and at 3 mg/ml for IP and PO injection. For IV injections, 5 mg/kg of XL01126 was administered into the tail vein. For IP and PO injections, 30 mg/kg of XL01126 was administered via intraperitoneal injection or oral gavage, respectively. The animals were restrained manually at the designated time points (0.083, 0.25, 0.5, 1, 2, 4, and 8 h); approximately, 110 μl of blood sample was collected via facial vein into K2EDTA tubes. Three mice per time point were used, resulting in a total of 21 mice for each administration route. The blood sample was put on ice and centrifuged at 2000g for 5 min to obtain the plasma sample within 15 min. The plasma, brain, CSF samples were stored at approximately -70 °C until analysis.