143703-25-7

生物活性靶点体外研究体内研究 143703-25-7 试剂级价格

143703-25-7

CAS号:143703-25-7
英文名:CE3F4
中文名:143703-25-7
CBNumber:CB33152589
分子式:C11H10Br2FNO
分子量:351.01
MOL File:143703-25-7.mol

143703-25-7化学性质

储存条件 :Store at -20°C
溶解度 :Soluble in DMSO > 10 mM
形态 :Powder
颜色 :White to off-white

143703-25-7性质、用途与生产工艺

生物活性 CE3F4 是一种选择性的 Epac1 拮抗剂，对 Epac1 和 Epac2(B) 的 IC50 值分别为 10.7 μM 和 66 μM。
靶点

IC50: 10.7 μM (Epac1), 66 μM (Epac2(B))
体外研究

CE3F4 is a selective antagonist of Epac1, with IC ₅₀ s of 10.7 μM and 66 μM for Epac1 and Epac2(B), respectively. CE3F4 is more active on Epac1 than (S)-stereoisomer ((S)-CE3F4, IC ₅₀ , 56 μM), but less active than (R)-CE3F4 (IC ₅₀ , 5.8 μM). CE3F4 (50 μM) shows more inhibitory activities against GEF activity of Epac1, than that of Epac2(AB) or Epac2(B). CE3F4 reduces the exchange activity of Epac1 induced by 007, with IC ₅₀ of 23 ± 3 μM. CE3F4 (40 μM) specifically inhibits Epac1 guanine nucleotide exchange activity without interference with Rap1 activity or Epac1-Rap1 interaction. CE3F4 has no influence on PKA activity. CE3F4 (20 μM) inhibits Epac-induced Rap1 activation in living cultured HEK293 cells. CE3F4 (20 μM) significantly inhibits the late phase of ERK activation stimulated by glucose in INS-1 cells.

体内研究

CE3F4 (1-3 mg/kg; through a catheter in the internal jugular vein) inhibits atrial fibrillation (AF) and CE3F4 (3 mg/kg; i.v.) inhibits ventricular arrhythmias.
CE3F4 (10 mg/kg; i.v.) improves cardiac function after myocardial infarction in mice.

Animal Model:	Wild-type (WT) mice (induced AF after 20min of CE3F4 administration)
Dosage:	3 mg/kg and 1mg/kg
Administration:	Through a catheter in the internal jugular vein
Result:	Shortened the duration of the pacing-induced AF at 3mg/kg.

Animal Model:	Casq2-KO mice (premature ventricular contraction induced by isoproterenol injection 20min after CE3F4 administration)
Dosage:	3 mg/kg
Administration:	I.v.
Result:	Reduced the incidence of sympathetic activation-induced ventricular arrhythmias.