受注:045-509-1970 |
技術サポート:[email protected] 平日9:00〜18:00 1営業日以内にご連絡を差し上げます |
Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
|
化学式 | C20H24FN5O3 |
|||
分子量 | 401.43 | CAS No. | 873697-71-3 | |
Solubility (25°C)* | 体外 | DMSO | 80 mg/mL (199.28 mM) | |
Ethanol | 6 mg/mL (14.94 mM) | |||
Water | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | 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. [1] 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. [1] |
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. [1] 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. [2] |
キナーゼアッセイ | Biochemical assays | |
---|---|---|
Cardiac S1 myosin and thin filament proteins (actin, troponin complex, and tropomyosin) are prepared from bovine heart or rabbit skeletal muscle. Smooth muscle myosin is prepared from chicken gizzard. ATPase assays are performed in a kinetic fashion using NADH coupled enzyme system at pCa2+ = 6.75. Rates are normalized to a DMSO control. | ||
動物実験 | 動物モデル | Sprague Dawley rats. |
投薬量 | ≤1.2 mg/kg/hour | |
投与方法 | Administered via i.v. |
|
Data from [Data independently produced by University of Illinois at Chicago, 2014]
Data from [Data independently produced by , , J Physiol, 2018, 596(1):31-46]
The force of the myosin motor sets cooperativity in thin filament activation of skeletal muscles [ Commun Biol, 2022, 5(1):1266] | PubMed: 36400920 |
Effects of omecamtiv mecarbil and mavacamten in isolated human atrium [ Naunyn Schmiedebergs Arch Pharmacol, 2022, 10.1007/s00210-022-02333-0] | PubMed: 36399186 |
Myosin with hypertrophic cardiac mutation R712L has a decreased working stroke which is rescued by omecamtiv mecarbil [ Elife, 2021, 10e63691] | PubMed: 33605878 |
Mechanistic analysis of actin-binding compounds that affect the kinetics of cardiac myosin-actin interaction [ J Biol Chem, 2021, S0021-9258(21)00245-3] | PubMed: 33639160 |
Generative adversarial networks for construction of virtual populations of mechanistic models: simulations to study Omecamtiv Mecarbil action [ J Pharmacokinet Pharmacodyn, 2021, 10.1007/s10928-021-09787-4] | PubMed: 34716531 |
Development and Application of NovelIn VitroAssays to Advance Drug Discovery for Arrhythmogenic Cardiomyopathy and Respiratory Syncytial Virus Infection [ ProQuest , 2021, 28718834] | PubMed: none |
Orthophosphate increases the efficiency of slow muscle-myosin isoform in the presence of omecamtiv mecarbil [ Nat Commun, 2020, 11(1):3405] | PubMed: 32636378 |
Sarcomere integrated biosensor detects myofilament-activating ligands in real time during twitch contractions in live cardiac muscle [ J Mol Cell Cardiol, 2020, 147:49-61] | PubMed: 32791214 |
Phosphorylation of Cardiac Myosin-Binding protein-C Contributes to Calcium Homeostasis [ J Biol Chem, 2020, jbc.RA120.13296] | PubMed: 32554466 |
SarcTrack: An Adaptable Software Tool for Efficient Large-Scale Analysis of Sarcomere Function in hiPSC-Cardiomyocytes [Toepfer CN, et al. Circ Res, 2019, 10.1161/CIRCRESAHA.118.314505] | PubMed: 30700234 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。