DG-041 是高亲和力，选择性的，有效的EP3受体拮抗剂，在结合和 FLIPR 试验中，IC50分别为 4.6 nM 和 8.1 nM。DG-041通过抑制PGE2促进血小板聚集。DG-041具有血脑屏障渗透性。
产品描述
DG-041 is an antagonist of high affinity EP3 receptor (IC50s: 4.6 nM and 8.1 nM in the binding and FLIPR assay, respectively ). DG-041 inhibits PGE2 facilitation of platelet aggregation and it also crosses the blood-brain barrier.
体外活性
DG-041 was a less effective the DP1 (IC50: 131 nM), EP1 (IC50: 486 nM) and TP receptors (IC50: 742 nM) antagonist [1].
体内活性
DG-041 has CL of 1250 mL/h/kg for intravenous. DG-041 (1.78 mg/kg for i.v or 9.62 mg/kg for p.o) has t1/2 of 2.7 hours, 4.06 hours. DG-041 (1.78 mg/kg for i.v or 9.62 mg/kg for p.o) has Cmax of 9.46 μM, 2.74 μM for intravenous and oral administration, respectively [1].
Cas No.
861238-35-9
分子式
C23H15Cl4FN2O3S2
分子量
592.32
储存和溶解度
DMSO:55 mg/ml (92.86 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
