NDT 9513727

NDT 9513727 is a potent, selective, orally active and competitive inverse agonist of the human C5aR (C5a receptor), with an IC₅₀ of 11.6 nM. NDT 9513727 can be used for the research of human inflammatory diseases^[1]. IC50 & Target: IC50: 11.6 nM (human C5aR)^[1] In Vitro: NDT 9513727 inhibits C5a-stimulated responses, including guanosine 5'-3-O-(thio)triphosphate binding, Ca²⁺ mobilization, oxidative burst, degranulation, cell surface CD11b expression and chemotaxis in various cell types with IC₅₀s from 1.1 to 9.2 nM, respectively^[1].
In Vivo: NDT 9513727 (3-30 mg/kg; p.o.) exhibits a dose-dependent inhibition of hC5a-induced neutropenia^[1].
NDT 9513727 exhibits moderate oral bioavailability (rat 73%, monkey 26%) and C_max (rat 5.98 μM, monkey 830 nM) following oral administration (rat 50, monkey 25.2 mg/kg)^[1].
NDT 9513727 exhibits moderate plasma elimination half-lives (rat 4.8, monkey 7.9 h) due to low plasma clearance (1.4 L/h/kg and 3.8 L/h/kg respectively) following oral administration (rat 50, monkey 25.2 mg/kg)^[1].