| Bioactivity | AE-3763 is a peptide-based human neutrophil elastase inhibitor with an IC50 of 29 nM. | ||||||||||||
| Target | IC50: 29 nM (Human neutrophil elastase) | ||||||||||||
| Invitro | AE-3763 exhibits potent in vitro inhibitory activity against human neutrophil elastase as well as extremely high solubility and stability in water[1]. | ||||||||||||
| In Vivo | Edema and leukocytes infiltration into the lung are significantly inhibited by infusion of AE-3763. AE3763 significantly improves survival rate by 24 h in a mouse model of fatal shock associated with multiple organ dysfunction. AE-3763 dose-dependently prevents hemorrhage when given intravenously by infusion (ED50: 0.42 mg/kg/h) or by bolus injection (1.2 mg/kg). With regard to the toxicity of AE-3763 in mice, the results of a preliminary study have shown no overt toxic effect even at the high dose of 300 mg/kg, iv[1]. | ||||||||||||
| Name | AE-3763 | ||||||||||||
| CAS | 291778-77-3 | ||||||||||||
| Formula | C23H34F3N5O7 | ||||||||||||
| Molar Mass | 549.54 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Inoue Y, et al. Development of a highly water-soluble peptide-based human neutrophil elastase inhibitor; AE-3763 for treatment of acute organ injury. Bioorg Med Chem. 2009 Nov 1;17(21):7477-86. |