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Chemical Structure| 113559-13-0 Chemical Structure| 113559-13-0

Structure of E-4031
CAS No.: 113559-13-0

Chemical Structure| 113559-13-0

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E-4031 is a benzenesulfonamide antiarrhythmic agent which blocks the ATP-sensitive potassium channel.

Synonyms: E-4031 dihydrochloride; E-4031 (hydrochloride)

4.5 *For Research Use Only! Not for Human Use. We Do Not Sell to Patients.

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Product Details of E-4031

CAS No. :113559-13-0
Formula : C21H29Cl2N3O3S
M.W : 474.44
SMILES Code : CS(=O)(NC1=CC=C(C(C2CCN(CCC3=NC(C)=CC=C3)CC2)=O)C=C1)=O.[H]Cl.[H]Cl
Synonyms :
E-4031 dihydrochloride; E-4031 (hydrochloride)
English Name :N-(4-(1-(2-(6-Methylpyridin-2-yl)ethyl)piperidine-4-carbonyl)phenyl)methanesulfonamide dihydrochloride
MDL No. :MFCD01754739
InChI Key :ZQBNWMFBOSOOLX-UHFFFAOYSA-N
Pubchem ID :3087190

Safety of E-4031

Related Pathways of E-4031

RTK
JAK-STAT

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Non-pregnant mouse uterine smooth muscle cells 1 μM 20 minutes increased spontaneous contractile activity J Physiol. 2009 May 15;587(Pt 10):2313-26.
Rabbit left ventricular cardiomyocytes 20 nmol/L 20 minutes E-4031 significantly prolonged MAPD90 and increased BVR, and this effect was more pronounced at slower pacing rates. Circulation. 2011 Apr 26;123(16):1713-20
Chinese hamster ovary cells 5 µmol/l Block I_Kr current to study the effect of E3 on HERG current J Clin Invest. 2002 Apr;109(8):1083-90
rabbit ventricular myocytes 5 μM selectively block HERG/IKr current to study its role in repolarization J Clin Invest. 1999 Mar;103(6):889-96
human induced pluripotent stem cell-derived cardiomyocytes (hiPSC-CMs) 1 mmol/L 15 minutes E-4031 terminated tachycardia episodes by inhibiting hERG potassium channels with 100% efficacy. Cardiovasc Res. 2020 Jul 1;116(8):1487-1499

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
New Zealand White rabbits Isolated heart model Perfusion 20 nmol/L Pacing cycle lengths from 400 to 2000 ms, each rate for 3-4 minutes E-4031 significantly prolonged MAPD90 and increased BVR, and this effect was more pronounced at slower pacing rates. TTX significantly attenuated the RRD effects of E-4031 on MAPD90 and BVR and abolished TdP induced by E-4031. Circulation. 2011 Apr 26;123(16):1713-20

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.11mL

0.42mL

0.21mL

10.54mL

2.11mL

1.05mL

21.08mL

4.22mL

2.11mL

Dissolving Methods
The prepared working fluid is recommended to be prepared now and used up as soon as possible in a short period of time. The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1

References

 

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