| Identification | Back Directory | [Name]
NDT 9513727 | [CAS]
439571-48-9 | [Synonyms]
NDT 9513727
N,N-Bis(1,3-benzodioxol-5-ylmethyl)-1-butyl-2,4-diphenyl-1H-Imidazole-5-methanamine | [Molecular Formula]
C36H35N3O4 | [MDL Number]
MFCD22683794 | [MOL File]
439571-48-9.mol | [Molecular Weight]
573.68 |
| Chemical Properties | Back Directory | [Boiling point ]
723.1±62.0 °C(Predicted) | [density ]
1.23±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: 100 mM; Ethanol: 100 mM | [form ]
A solid | [pka]
6.69±0.50(Predicted) | [color ]
White to yellow |
| Hazard Information | Back Directory | [Description]
NDT 9513727 is a competitive antagonist of the C5a receptor (C5aR; IC50 = 11.6 nM for human recombinant receptors) that has inverse agonist activity in a GTPγ[35S] assay. It is selective for human recombinant over rat and mouse recombinant C5aRs (IC50 = >10 μM for both) but does have activity at macaque and gerbil receptors (IC50s = 7.3 and 6.4 nM, respectively). NDT 9513727 inhibits degranulation in U937 cells stimulated with C5a (IC50 = 7.1 nM). It also prevents neutropenia induced by human recombinant C5a in gerbils (ED50 = 2.2 mg/kg) and in cynomolgus macaques when administered at doses of 5 and 25 mg/kg. | [Uses]
NDT 9513727 is a selective, and potent inverse agonist of the human C5aR. NDT 9513727 has been shown to effectively inhibit C5a-induced neutropenia in gerbil and cynomolgus macaque in vivo. These results suggest that NDT 9513727 is a promising candidate for the treatment of human inflammatory diseases. | [storage]
Store at +4°C |
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