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CE3F4 

Cat. No.: HY-108539 Purity: 98.39%
Handling Instructions

CE3F4 is a selective antagonist of exchange protein directly activated by cAMP (Epac1), with IC50s of 10.7 μM and 66 μM for Epac1 and Epac2(B), respectively.

For research use only. We do not sell to patients.

CE3F4 Chemical Structure

CE3F4 Chemical Structure

CAS No. : 143703-25-7

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10 mM * 1 mL in DMSO USD 72 In-stock
Estimated Time of Arrival: December 31
5 mg USD 65 In-stock
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10 mg USD 120 In-stock
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50 mg USD 500 In-stock
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100 mg USD 850 In-stock
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Description

CE3F4 is a selective antagonist of exchange protein directly activated by cAMP (Epac1), with IC50s of 10.7 μM and 66 μM for Epac1 and Epac2(B), respectively.

IC50 & Target

IC50: 10.7 μM (Epac1), 66 μM (Epac2(B))[1]

In Vitro

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)[1]. 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[2]. CE3F4 (20 μM) significantly inhibits the late phase of ERK activation stimulated by glucose in INS-1 cells[3].

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

In Vivo

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[4].
CE3F4 (10 mg/kg; i.v.) improves cardiac function after myocardial infarction in mice[5].

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

Animal Model: Wild-type (WT) mice (induced AF after 20min of CE3F4 administration)[4]
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)[4]
Dosage: 3 mg/kg
Administration: I.v.
Result: Reduced the incidence of sympathetic activation-induced ventricular arrhythmias.
Molecular Weight

351.01

Formula

C₁₁H₁₀Br₂FNO

CAS No.

143703-25-7

SMILES

O=CN1C(C)CCC2=C1C=C(Br)C(F)=C2Br

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, stored under nitrogen

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

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (142.45 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8489 mL 14.2446 mL 28.4892 mL
5 mM 0.5698 mL 2.8489 mL 5.6978 mL
10 mM 0.2849 mL 1.4245 mL 2.8489 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (7.12 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (7.12 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (7.12 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 98.39%

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Keywords:

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