873697-71-3 Usage
Description
Omecamtiv mecarbil (CK-1827452) is a specific cardiac myosin activator and a clinical drug for left ventricular systolic heart failure. Phase 2.
In vitro
In vitro, Omecamtiv mecarbil selectively activates cardiac myosin by increasing the myosin ATPase rate. In isolated cardiac myocytes, Omecamtiv mecarbil results in increase of myocyte contractility and overcomes of the myosin inhibitor BDM without increasing the calcium transient or inhibiting the PDE pathway. [
In vivo
Omecamtiv mecarbil significantly increases fractional shortening starting at 0.4 mM plasma concentrations in SD rats, sham animals and in rats with heart failure. In conscious dogs with myocardial infarction (MI-sHF), Omecamtiv mecarbil leads to a significant increase in wall thickening (25%), stroke volume (44%), cardiac output (22%) and left ventricular (LV) systolic ejection time (26%). In addition, Omecamtiv mecarbil also results in the decreases of some hemodynamic parameters including heart rate, mean left atrial pressure, and LV end-diastolic pressure. In conscious dogs with left ventricular hypertrophy (LVH-sHF), Omecamtiv mecarbil leads to similar and not statistically different effects on hemodynamic parameters.
Uses
Different sources of media describe the Uses of 873697-71-3 differently. You can refer to the following data:
1. CK 1827452 is a promising new drug in systolic heart failure. It accelerates the transition of myosin into the force-generating state without affecting cardiac myocyte calcium homeostasis. CK 1827452
increases cardiac function by increasing the duration of ejection without changing the rates of contraction.
2. CK 1827452 is a promising new drug in systolic heart failure. It accelerates the transition of myosin into the force-generating state without affecting cardiac myocyte calcium homeostasis. CK 1827452 increases cardiac function by increasing the duration of ejection without changing the rates of contraction.
Biological Activity
omecamtiv mecarbil (ck-1827452) is the first potent cardiac myosin activator that can specifically activate the cardiac myosin s1 domain but not other muscle myosins. in
references
1. malik fi1, hartman jj, elias ka, morgan bp, rodriguez h, brejc k, anderson rl, sueoka sh, lee kh, finer jt, sakowicz r, baliga r, cox dr, garard m,godinez g, kawas r, kraynack e, lenzi d, lu pp, muci a, niu c, qian x, pierce dw, pokrovskii m, suehiro i, sylvester s, tochimoto t, valdez c, wang w,katori t, kass da, shen yt, vatner sf, morgans dj. cardiac myosin activation: a potential therapeutic approach for systolic heart failure. science. 2011 mar 18;331(6023):1439-43.
Check Digit Verification of cas no
The CAS Registry Mumber 873697-71-3 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 8,7,3,6,9 and 7 respectively; the second part has 2 digits, 7 and 1 respectively.
Calculate Digit Verification of CAS Registry Number 873697-71:
(8*8)+(7*7)+(6*3)+(5*6)+(4*9)+(3*7)+(2*7)+(1*1)=233
233 % 10 = 3
So 873697-71-3 is a valid CAS Registry Number.
873697-71-3Relevant articles and documents
ALTERNATE PROCESSES FOR THE PREPARATION OF OMECAMTIV MECARBIL
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, (2021/04/17)
Aspects of the present application relate to process for the preparation of Omecamtiv mecarbil and salts thereof. Specific aspects relate to novel urea intermediate, preparative process thereof and its use in the preparation of Omecamtiv mecarbil and salts thereof. The improved process for the preparation of Omecamtiv mecarbil are industrially viable.
SYNTHESIS OF OMECAMTIV MECARBIL
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, (2019/01/17)
Provided herein is a synthesis for omecamtiv mecarbil dihydrochloride hydrate and various intermediates. (I)
Synthesis of unsymmetrical diarylureas via Pd-catalyzed C-N cross-coupling reactions
Breitler, Simon,Oldenhuis, Nathan J.,Fors, Brett P.,Buchwald, Stephen L.
supporting information; experimental part, p. 3262 - 3265 (2011/08/07)
A facile synthesis of unsymmetrical N,N′-diarylureas is described. The utilization of the Pd-catalyzed arylation of ureas enables the synthesis of an array of diarylureas in good to excellent yields from benzylurea via a one-pot arylation-deprotection protocol, followed by a second arylation.
