NDT 9513727
Chemical Name: N,N-Bis(1,3-benzodioxol-5-ylmethyl)-1-butyl-2,4-diphenyl-1H-Imidazole-5-methanamine
Purity: ≥98%
Biological Activity
NDT 9513727 is a potent C5a receptor (C5aR) negative allosteric modulator (NAM) (IC50 = 11.6 nM); selective for human C5aR (IC50 values for rat and mouse C5aR are > 10 μM). Exhibits inverse agonist pharmacokinetics. Blocks degranulation response in C5a-stimulated U937 cells (IC50 = 7.1 nM). Exhibits selectivity for primate and gerbil receptor over other species. Orally bioavailable.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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The Novel Receptor C5aR2 Is Required for C5a-Mediated Human Mast Cell Adhesion, Migration, and Proinflammatory Mediator Production.
Pundir P, MacDonald C, Kulka M
J Immunol, 2015;195(6):2774-87. -
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.
Brodbeck et al.
J.Pharmacol.Exp.Ther., 2008;327:898 -
Structure of the complement C5a receptor bound to the extra-helical antagonist NDT9513727.
Robertson
Nature, 2018;553:111
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Citation for NDT 9513727
The citations listed below are publications that use Tocris products. Selected citations for NDT 9513727 include:
1 Citation: Showing 1 - 1
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Orthosteric and allosteric action of the C5a receptor antagonists.
Authors: Liu
Nat Struct Mol Biol 2018;25:472
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