NDT 9513727

Research use only, not for human use.

NDT 9513727 is a potent, selective and orally bioavailable C5a receptor inverse agonist with IC50 of 11.6 nM in radioligand binding assay.

NDT 9513727 is a potent, selective and orally bioavailable C5a receptor inverse agonist with IC50 of 11.6 nM in radioligand binding assay; exhibits potent activity in both gerbil and monkey lung membrane preparations (6.4 and 7.3 nM), but has minimal activity in rat, mouse, and dog lung preparations (>10 uM); blocks hC5a-stimulated chemotaxis activity in human polymorphonuclear neutrophils and U937 cells with IC50 of 4.7 and 4.3 nM, respectively, inhibits C5a-stimulated responses, including guanosine 5'-3-O-(thio)triphosphate binding, Ca(2+) mobilization, oxidative burst, degranulation, cell surface CD11b expression and chemotaxis in various cell types with IC50 of 1.1-9.2 nM; effectively inhibits C5a-induced neutropenia in gerbil and cynomolgus macaque in vivo.

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Animal Model:Six-week-old Mongolian gerbils Dosage:1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg Administration:Oral administration Result:Significantly inhibited hC5a-induced neutropenia at 3 mg/kg, 10 mg/kg, 30 mg/kg.Animal Model:Rat Dosage:50 mg/kg (Pharmacokinetic Analysis) Administration:Oral administrationResult:Oral bioavailability (73%), Cmax (5.98 μM), T1/2 (4.8 h).Animal Model:Monkey Dosage:25.2 mg/kg (Pharmacokinetic Analysis) Administration:Oral administrationResult:Oral bioavailability (26%), Cmax (830 nM), T1/2 (7.9 h).

NDT9513727

Immunology/Inflammation

Complement System

Complement System

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439571-48-9

573.693

C36H35N3O4

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (174.31 mM)

CCCCN1C(CN(CC2=CC=C(OCO3)C3=C2)CC4=CC=C(OCO5)C5=C4)=C(C6=CC=CC=C6)N=C1C7=CC=CC=C7

N,N-Bis(1,3-benzodioxol-5-ylmethyl)-1-butyl-2,4-diphenyl-1H-imidazole-5-methanamine

(-20℃)

With Ice Pack

≥ 2 years