| Identification | Back Directory | [Name]
CE3F4 | [CAS]
143703-25-7 | [Synonyms]
CE3F4
CE3F4 >=98% (HPLC)
5,7-Dibromo-6-fluoro-3,4-dihydro-2-methyl-1(2H)-quinolinecarboxaldehyde
1(2H)-Quinolinecarboxaldehyde, 5,7-dibromo-6-fluoro-3,4-dihydro-2-methyl- | [Molecular Formula]
C11H10Br2FNO | [MOL File]
143703-25-7.mol | [Molecular Weight]
351.01 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO > 10 mM | [form ]
Powder | [color ]
White to off-white | [InChI]
InChI=1S/C11H10Br2FNO/c1-6-2-3-7-9(15(6)5-16)4-8(12)11(14)10(7)13/h4-6H,2-3H2,1H3 | [InChIKey]
ZZLQPWXVZCPUGC-UHFFFAOYSA-N | [SMILES]
N1(C=O)C2=C(C(Br)=C(F)C(Br)=C2)CCC1C |
| Hazard Information | Back Directory | [Uses]
CE3F4 has been used as a selective exchange protein directly activated by cAMP isoform 1 (Epac1) inhibitor in cell proliferation assay to study the influence of Epac type I on cell proliferation of C6 cells (a model of glioma). | [Biological Activity]
CE3F4 is a tetrahydroquinoline derivative th at blocks agonist-stimulated Epac1 (exchange protein directly activated by cAMP isoform 1) guanine nucleotide exchange activity toward its effector Rap1 (IC50 = 23 μM; Epac agonist = 2 μM 8-CPT-2μ-O-Me-cAMP) by targeting agonist-bound Epac1 in an agonist-uncompetitive manner without affecting the GDP exchange on Rap1Rap1-Epac1 interactionor PKA type I/II activity (CβRIβ & CαRIIβ). CE3F4 (20 μM) effectively inhbits cellular Rap1 activation upon 10 μM Sp-8-pCPT-2μ-O-Me-cAMPS (Epac1-transfected HEK293 and r at neonatal cardiac myocytes) or 10 μM β-adrenergic receptor agonist isoprenaline stimulation (β1AR & Epac1 dually transfected HEK293). The isolated CE3F4 R enantiomer is reported to display 10-fold Epac1 selectivity over Epac2and is 10-times more potent than the CE3F S enantiomer against Epac1.''Epac1 is a downstream effector of the cyclic adenosine monophosp | [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]. | 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.
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| 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.
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| [storage]
Store at -20°C |
|
| Company Name: |
BOC Sciences
|
| Tel: |
|
| Website: |
https://www.bocsci.com |
| Company Name: |
Energy Chemical
|
| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
|