Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C24H21FN4O2S |
| Molecular Weight | 448.513 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CS(=O)(=O)NC1=CC=CC(=N1)[C@@H](C(C2=CC=CN=C2)C3=CC=CN=C3)C4=CC=C(F)C=C4
InChI
InChIKey=QPWKXYZJANVPLF-DEOSSOPVSA-N
InChI=1S/C24H21FN4O2S/c1-32(30,31)29-22-8-2-7-21(28-22)24(17-9-11-20(25)12-10-17)23(18-5-3-13-26-15-18)19-6-4-14-27-16-19/h2-16,23-24H,1H3,(H,28,29)/t24-/m0/s1
| Molecular Formula | C24H21FN4O2S |
| Molecular Weight | 448.513 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
Approval Year
| Substance Class |
Chemical
Created
by
admin
on
Edited
Mon Mar 31 22:45:10 GMT 2025
by
admin
on
Mon Mar 31 22:45:10 GMT 2025
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| Record UNII |
HR3DSH1839
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| Record Status |
Validated (UNII)
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| Record Version |
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HR3DSH1839
Created by
admin on Mon Mar 31 22:45:10 GMT 2025 , Edited by admin on Mon Mar 31 22:45:10 GMT 2025
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875562-81-5
Created by
admin on Mon Mar 31 22:45:10 GMT 2025 , Edited by admin on Mon Mar 31 22:45:10 GMT 2025
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11525190
Created by
admin on Mon Mar 31 22:45:10 GMT 2025 , Edited by admin on Mon Mar 31 22:45:10 GMT 2025
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PRIMARY |
| Related Record | Type | Details | ||
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ACTIVE MOIETY |
Mechanism of Action: Undefined mechanism; Highest Development Phase: Discontinued for Cardiovascular disorders; Most Recent Event: 05 Jul 2006 Phase-I clinical trials in Cardiovascular disorders in USA (unspecified route)
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ACTIVE MOIETY |
We evaluated the viability of IKur as a target for maintenance of sinus rhythm in patients with a history of atrial fibrillation through the testing of MK-0448, a novel IKur inhibitor. These data led to a 2-part first-in-human study: Part I evaluated safety and pharmacokinetics, and part II was an invasive electrophysiological study in healthy subjects. MK-0448 was well-tolerated with mild adverse experiences, most commonly irritation at the injection site. During the electrophysiological study, ascending doses of MK-0448 were administered, but
no increases in atrial or ventricular refractoriness were detected, despite achieving plasma concentrations in excess of 2 .MU.mol/L. The contribution of IKur to human atrial electrophysiology is less prominent than in preclinical models and therefore is likely to be of limited therapeutic value for the prevention of atrial fibrillation.
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![Structure of N-[6-[(1S)-1-(4-Fluorophenyl)-2,2-di-3-pyridinylethyl]-2-pyridinyl]methanesulfonamide](/img/d6a089d3-d53a-4336-8b6b-79afd0df33c8.svg "Structure of N-[6-[(1S)-1-(4-Fluorophenyl)-2,2-di-3-pyridinylethyl]-2-pyridinyl]methanesulfonamide")