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。

CE3F4 is a selective antagonist of exchange protein directly activated by cAMP (Epac1), with IC 50 s of 10.7 μM and 66 μM for Epac1 and Epac2(B), respectively.

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IC50: 10.7 μM (Epac1), 66 μM (Epac2(B))

CE3F4 is a selective antagonist of Epac1, with IC50s of 10.7 μM and 66 μM for Epac1 and Epac2(B), respectively. CE3F4 is more active on Epac1 than (S)-stereoisomer ((S)-CE3F4, IC50, 56 μM), but less active than (R)-CE3F4 (IC50, 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 IC50 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.

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. has not independently confirmed the accuracy of these methods. They are for reference only.

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-20°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

[1]. Courilleau D, et al. The (R)-enantiomer of CE3F4 is a preferential inhibitor of human exchange protein directly activated by cyclic AMP isoform 1 (Epac1). Biochem Biophys Res Commun. 2013 Oct 25;440(3):443-8.
[2]. Courilleau D, et al. Identification of a tetrahydroquinoline analog as a pharmacological inhibitor of the cAMP-binding protein Epac. J Biol Chem. 2012 Dec 28;287(53):44192-202.

In Vitro: DMSO : 50 mg/mL (142.45 mM; Need ultrasonic)配制储备液