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编 号:F743579
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1mg
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5mg
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生物活性:
Inclacumab (Anti-Human selectin P Recombinant Antibody) is a human monoclonal IgG4 antibody selectively targets P-selectin with a Kd value of 9.9 nM. Inclacumab inhibits P-selectin glycoprotein ligand 1 (PSGL-1) mimetic peptide bind with P-selectin with an IC50 value of 1.9 μg/mL and strongly inhibits cell adhesion.

体内研究:
Inclacumab (4 mg/kg; s.c. once) reduces TRAP- and ADP-induced PLA levels in cynomolgus monkeys.Inclacumab (2-50 mg/kg; i.v.; once a week for 13 weeks) inhibits TRAP induced PLA levels in cynomolgus monkeys.Animal Model:Cynomolgus monkeys
Dosage:4 mg/kg
Administration:Subcutaneous injection; 4 mg/kg; once
Result:Significantly reduced TRAP-induced PLA levels from 25% to 6% and supressed PLA formation ≥80% for at least 28 days post treatment. Remained plasma concentrations >20 μg/mL during post treatment for 28 days. Significantly inhibited the formation of ADP (10 μM)-induced PLAs.
Animal Model:Cynomolgus monkeys
Dosage:2, 10, and 50 mg/kg
Administration:Intravenous injection; once daily; for 13 weeks
Result:Inhibited TRAP-induced PLA and remained concentrations at all three dose levels are higher than 20 μg/mL. Persisted the full inhibition of PLA formation between dosing period.

体外研究:
Inclacumab (0.4-40 μg/mL; 5 min) significantly reduces flow adhesion of P-Selectin with Whole Blood (WB) and isolated White Blood Cell (I-WBC) and shows a morestronger effect on isolated white cells.Inclacumab shows great binding affinity to P-selectin with a Kd value of 9.9 nM.Inclacumab inhibits PSGL-1 mimetic peptide binding with P-selectin with an IC50 value of 1.9 μg/mL.Inclacumab blocks the adhesion of PSGL-1 expressing cells to an immobilized P-selectin with an IC50 value of 430 ng/mL.Inclacumab (0-100 μg/mL; 5min) dose-dependently inhibits thrombin receptor-activating peptide (TRAP)-induced platelet-leukocyte aggregates (PLA) levels with an IC50 value of 1.4 μg/mL.
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