ASP7657 free base_product_DataBase

Bioactivity	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].
Invitro	ASP7657 free base 抑制 CHO 细胞 (表达大鼠 EP4 受体) 和人淋巴母细胞样 T 细胞中 PGE2 诱导的 cAMP 增加，IC50 值分别为 0.86 nM 和 0.29 nM[1]。
In Vivo	ASP7657 (0.1 mg/kg，口服，大鼠) 显示出 t1/2 为 1.38 h，Cmax 为 22.4 ng/mL，口服生物利用度为 46.2%[1].ASP7657 (0.003-0.1 mg/kg，口服) 抑制 LPS (1 μg/mL) 诱导的大鼠的全血中 TNF-α 释放[1]。ASP7657 (0.01 mg/kg，口服) 减少 2 型糖尿病小鼠中的尿白蛋白排泄[1]。 Animal Model:
Name	ASP7657 free base
CAS	1196045-28-9
Formula	C28H26F3N3O3
Molar Mass	509.52
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[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.

PeptideDB