| Identification | Back Directory | [Name]
3-Pyridinecarboxylic acid, 2-[4-[(2,3,4-trimethoxyphenyl)methyl]-1-piperazinyl]ethyl ester, hydrochloride (1:3) | [CAS]
2311824-72-1 | [Synonyms]
Ninerafaxstat 3HCl
Ninerafaxstat trihydrochloride
3-Pyridinecarboxylic acid, 2-[4-[(2,3,4-trimethoxyphenyl)methyl]-1-piperazinyl]ethyl ester, hydrochloride (1:3) | [Molecular Formula]
C22H30ClN3O5 | [MOL File]
2311824-72-1.mol | [Molecular Weight]
451.95 |
| Hazard Information | Back Directory | [Uses]
Ninerafaxstat trihydrochloride (IMB-1018972 trihydrochloride) is the trihydrochloride salt form of Ninerafaxstat (HY-139577). Ninerafaxstat trihydrochloride is a novel orally active cardiac mitochondrial drug that restores myocardial energy homeostasis. Ninerafaxstat trihydrochloride competitively inhibits 3-ketoacyl-CoA thiolase (3-KAT) to partially suppress fatty acid oxidation, and shifts cardiac energy metabolism from free fatty acid oxidation to glucose oxidation, regulating myocardial substrate utilization and thereby improving cardiac efficiency. Ninerafaxstat trihydrochloride can be used for research on cardiovascular diseases[1][2]. | [in vivo]
Ninerafaxstat trihydrochloride (30 mg/kg; once daily; 4 weeks; via osmotic minipump) can improve left ventricular systolic function and reduce left ventricular end diastolic pressure (LVEDP) and myocardial fibrosis in a mouse model of heart failure after myocardial infarction[2]. | Animal Model: | Murine model of post-MI HF[2]. | | Dosage: | 30 mg/kg | | Administration: | Via osmotic minipump; once daily; 4 weeks | | Result: | Increased left ventricular ejection fraction (LVEF) and reduced cardiac fibrosis. |
| [References]
[1] Moritz Hundertmark MD, et al. Kiosk 11R-TC-08 - Ninerafaxstat Modulates Cardiac Energy Metabolism in Cardio-metabolic Syndromes: A Mechanistic, Hyperpolarized MR Trial. Journal of Cardiovascular Magnetic Resonance. 2024; 26: 100325.
[2] Paul Chamberlin, et al. IMB-1018792, A NOVEL FIRST-IN CLASS PARTIAL FATTY ACID OXIDATION INHIBITOR IMPROVES CARDIAC REMODELING AND FUNCTION POST-MYOCARDIAL INFARCTION. J Am Coll Cardiol. 2021 May 11;77(18):539. |
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