PK68 (5 mg/kg, 25 mg/kg; oral gavage; daily; for 7 days) or (2 mg/kg, i.v.; 10 mg/kg, p.o.; for 14 days) exhibits a favorable pharmacokinetic profile and no obvious toxicity in mice[1].
PK68 (1 mg/kg, i.p.) ameliorates TNF-induced systemic inflammatory response syndrome[1].
PK68 (5 mg/kg, i.v.) inhibits RIPK1 that results in attenuated tumor cell transmigration across the endothelial barrier and preventive suppression of tumor metastasis[1].
| Animal Model: | C57BL/6 mice[1] |
| Dosage: | 5 mg/kg, 25 mg/kg |
| Administration: | 5 mg/kg, 25 mg/kg; oral gavage; daily; for 7 days |
| Result: | Exhibited favorable pharmacokinetic profiles and no obvious toxicity in mice treated with a 14-day course at a dose of 25 mg/kg. |
| Animal Model: | C57BL/6 mice[1] |
| Dosage: | 2 mg/kg, 10 mg/kg |
| Administration: | 2 mg/kg, i.v.; 10 mg/kg, p.o; for 14 days |
| Result: | | PO (Gavage) | IV (Bolus) | | Tmax (hr) | 0.5 | | | Cmax (ng/mL) | 2423 | | | AUC0-24 (ng/mLhr) | 4821 | 1588 | | AUCINF (ng/mLhr) | 4897 | 1590 | | t1/2 (hr) | 1.3 | 1.0 | | MRT (hr) | 1.8 | 0.8 | | CL (mL/hr/kg) | | 1258 | | CL (mL/min/kg) | | 21 | | Vss (mL/kg) | | 1009 | | Vss (L/kg) | | 1.0 | | F(%) | 61 | | |
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| Animal Model: | C57BL/6 mice[1] |
| Dosage: | 1 mg/kg |
| Administration: | 1 mg/kg, i.p. |
| Result: | Provided effective protection against TNFα-induced lethal shock. |
| Animal Model: | C57BL/6 mice[1] |
| Dosage: | 5 mg/kg |
| Administration: | 5 mg/kg, i.v. |
| Result: | Significantly reduced the number of pulmonary metastasis nodules, decreased lung metastasis, decreased number of RFP-LL/2 cells, attenuated transmigration of RFP-LL/2 cells through the endothelial cell monolayer and had no obvious influence on the proliferation rate and invasion ability of B16-F10 or RFP-LL/2 cells without the endothelial cell monolayer in vitro. |