OMecaMtiv Mecarbil
OMecaMtiv Mecarbil Basic information
- Product Name:
- OMecaMtiv Mecarbil
- Synonyms:
-
- 1-Piperazinecarboxylic acid,4-[[2-fluoro-3-[[[(6-methyl-3-pyridinyl)amino]carbonyl]amino]phenyl]methyl]-, methyl ester
- OMecaMtiv Mecarbil
- OMecaMtiv Mecarbil (CK-1827452)
- CK1827452
- CK-1827452
- CK-1827452 (OMecaMtiv Mecarbil)
- CK 1827452O
- mecamtiv mecarbil
- CAS:
- 873697-71-3
- MF:
- C20H24FN5O3
- MW:
- 401.43
- EINECS:
- 850-774-6
- Product Categories:
-
- Inhibitors
- Mol File:
- 873697-71-3.mol
OMecaMtiv Mecarbil Chemical Properties
- Melting point:
- 180℃
- storage temp.
- -20°C Freezer
- solubility
- DMSO (Slightly), Methanol (Slightly)
- form
- Solid
- color
- White to Off-White
- Water Solubility
- 40.25mg/L at 25℃
- InChI
- InChI=1S/C20H24FN5O3/c1-14-6-7-16(12-22-14)23-19(27)24-17-5-3-4-15(18(17)21)13-25-8-10-26(11-9-25)20(28)29-2/h3-7,12H,8-11,13H2,1-2H3,(H2,23,24,27)
- InChIKey
- RFUBTTPMWSKEIW-UHFFFAOYSA-N
- SMILES
- N1(C(OC)=O)CCN(CC2=CC=CC(NC(NC3=CC=C(C)N=C3)=O)=C2F)CC1
- LogP
- -0.531
OMecaMtiv Mecarbil Usage And Synthesis
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
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.
Definition
ChEBI: Omecamtiv mecarbil is a member of ureas.
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
in vivo
Omecamtiv mecarbil (100-1000 ng/mL) demonstrates concentration-dependent increases in FS in Sprague?Dawley rats model. Omecamtiv mecarbil demonstrates good PK parameters in both rats (Sprague?Dawley) and dogs (Beagle) with clearances of 22 and 7.2 mL/min/kg, volumes of 3.5 and 3.6 L/kg, and bioavailabilities (F%) of 100 and 80%, respectively[1]. Omecamtiv mecarbil does not affect the phosphorylation status of myofilament proteins in both WT and KO hearts as shown by the absence of significant differences between pre and post Omecamtiv mecarbil samples within WT and KO groups, or affect the force generation at maximal Ca2+ activation (pCa 4.5) in any of the groups. Omecamtiv mecarbil increases the responsiveness of the cardiac myofilaments to Ca2+ at submaximal Ca2+-activations[2].
target
ATPase
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.
OMecaMtiv MecarbilSupplier
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- hanfangpharma@126.com; 18616537568
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- Product Name:Omecamtiv mecarbil
CAS:873697-71-3
Purity:98%+ Package:10g;100g;1kg;10kg
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- sales@boylechem.com
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- Product Name:CK1827452
CAS:873697-71-3
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- Product Name:CK 1827452
CAS:873697-71-3
Package:100Mg,10Mg,50Mg,5Mg
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- 0411-62910999 13889544652
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- Product Name:OMecaMtiv Mecarbil
CAS:873697-71-3
Purity:>98%,BR Package:50MG Remarks:4980
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- Products Intro
- Product Name:OMecaMtiv Mecarbil (CK-1827452)
CAS:873697-71-3
Purity:>99% Package:5Mg