Potent C5a receptor (C5aR) competitive antagonist (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.
|Storage||Store at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 573.68. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.74 mL||8.72 mL||17.43 mL|
|5 mM||0.35 mL||1.74 mL||3.49 mL|
|10 mM||0.17 mL||0.87 mL||1.74 mL|
|50 mM||0.03 mL||0.17 mL||0.35 mL|
References are publications that support the products' biological activity.
Brodbeck et al (2008) 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. 327 898 PMID: 18753409
Robertson (2018) Structure of the complement C5a receptor bound to the extra-helical antagonist NDT9513727. Nature 553 111 PMID: 29300009
If you know of a relevant reference for NDT 9513727, please let us know.
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Keywords: NDT 9513727, supplier, potent, complement, C5a, receptor, C5aR, antagonists, competitive, inverse, agonists, human, orally, active, NDT9513727, Complement, Complement, Tocris Bioscience
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