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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.
|Storage||Store at +4°C|
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.
|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 the degree 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 biological activity of the product.
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
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Keywords: NDT 9513727, NDT 9513727 supplier, potent, complement, C5a, receptor, C5aR, antagonists, competitive, inverse, agonists, human, orally, active, NDT9513727, NAM, negative, allostreic, modulators, Complement, 3333, Tocris Bioscience
1 Citation for NDT 9513727
Citations are publications that use Tocris products. Selected citations for NDT 9513727 include:
Liu (2018) Orthosteric and allosteric action of the C5a receptor antagonists. Nat Struct Mol Biol 25 472 PMID: 29867214
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