| Description | NDT 9513727 is a potent, selective and competitive C5aR1 inverse agonist for the study of inflammatory and immune disorders. |
| In vitro | NDT 9513727 抑制了 C5a 刺激引起的反应，包括鸟苷5'-3-O-(硫)三磷酸盐结合、钙离子释放、氧化爆发、颗粒脱颗粒、细胞表面 CD11b 表达和各种细胞类型的趋化作用，相应的 IC50 分别为1.1到9.2 nM[1]。 |
| In vivo | NDT 9513727（3-30 mg/kg）在天竺鼠和恒河猴体内有效抑制了 C5a 诱导的中性粒细胞减少[1]。 |
| Target activity | C5aR (human):11.6 nM |
| Synonyms | NDT9513727, NDT-9513727 |
| molecular weight | 573.68 |
| Molecular formula | C36H35N3O4 |
| CAS | 439571-48-9 |
| Storage | store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | Ethanol: 30 mg/mL (52.26 mM) DMSO: 80 mg/mL (139.37 mM), Sonication is recommended. |
| References | 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;327(3):898-909. 2. Brodbeck RM, Cortright DN, Kieltyka AP, Yu J, Baltazar CO, Buck ME, Meade R, Maynard GD, Thurkauf A, Chien DS, Hutchison AJ, Krause JE. Identification and characterization of NDT 9513727 [N,N-bis(1,3-benzodioxol-5-ylmethyl)-1-butyl-2,4-diphenyl-1H-imidazole-5-methanam ine], a novel, orally bioavailable C5a receptor inverse agonist. J Pharmacol Exp Ther. 2008 Dec;327(3):898-909. doi: 10.1124/jpet.108.141572. Epub 2008 Aug 27. PubMed PMID: 18753409. |