| Chemical Properties | Back Directory | [Boiling point ]
720.5±60.0 °C(Predicted) | [density ]
1.39±0.1 g/cm3(Predicted) | [solubility ]
DMF: 16.5mg/mL; DMSO: 16.5mg/mL; DMSO:PBS (pH 7.2) (1:3): 0.25mg/mL; Ethanol: 12.5mg/mL | [form ]
A crystalline solid | [pka]
4.82±0.10(Predicted) |
| Hazard Information | Back Directory | [Description]
ASP7657 is a novel, potent, and selective prostaglandin EP4 receptor antagonist. | [Uses]
ASP7657 free base is an orally active EP4 receptor antagonist, with Kis of 2.21 and 6.02 nM for the human and rat EP4 receptors[1]. | [in vivo]
ASP7657 free base (0.1 mg/kg, p.o., rats) shows a t1/2 of 1.38 h, Cmax of 22.4 ng/mL, and oral bioavailability of 46.2%[1].
ASP7657 free base (0.003-0.1 mg/kg, p.o.) inhibits LPS (1 μg/mL)-induced TNF-α release from rat whole blood[1].
ASP7657 free base (0.01 mg/kg, p.o.) attenuates urinary albumin excretion in type 2 diabetic mice[1].
| Animal Model: | LPS (1 μg/mL)-induced rats[1] | | Dosage: | 0.003, 0.01, 0.03, 0.1 mg/kg | | Administration: | p.o. | | Result: | Antagonized the PGE2-mediated inhibition of LPS-induced TNF-α release from rat whole blood culture, in a dose-dependent way. |
| [IC 50]
hEP4: 2.21 nM (IC50); rat EP4: 6.02 nM (IC50) | [References]
[1] Mizukami K, et al. Pharmacological properties of ASP7657, a novel, potent, and selective prostaglandin EP4 receptor antagonist. Naunyn Schmiedebergs Arch Pharmacol. 2018 Dec;391(12):1319-1326. DOI:10.1007/s00210-018-1545-x |
|
| Company Name: |
BOC Sciences
|
| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
|