| Bioactivity | 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]. | |||||||||
| Target | IC50: 11.6 nM (human C5aR) | |||||||||
| Invitro | 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 Cmax (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]. Animal Model: | |||||||||
| Name | NDT 9513727 | |||||||||
| CAS | 439571-48-9 | |||||||||
| Formula | C36H35N3O4 | |||||||||
| Molar Mass | 573.68 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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| Reference | [1]. Robbin M Brodbeck, et al. Identification and characterization of NDT 9513727 [N,N-bis(1,3-benzodioxol-5-ylmethyl)-1-butyl-2,4-diphenyl-1H-imidazole-5-methanamine], a novel, orally bioavailable C5a receptor inverse agonist. J Pharmacol Exp Ther. 2008 Dec;3 |
NDT 9513727
CAS: 439571-48-9 F: C36H35N3O4 W: 573.68
NDT 9513727 is a potent, selective, orally active and competitive inverse agonist of the human C5aR (C5a receptor), with
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