5mg Omecamtiv mecarbil （CK-1827452）/心肌肌球蛋白激動(dòng)劑
| 參考價(jià) | ￥ 1373 |
| 訂貨量 | ≥1 |
- 公司名稱 上海高創(chuàng)化學(xué)科技有限公司
- 品牌 Selleck
- 型號(hào) 5mg
- 產(chǎn)地 美國(guó)
- 廠商性質(zhì) 代理商
- 更新時(shí)間 2017/11/22 10:38:58
- 訪問(wèn)次數(shù) 1305
Omecamtiv mecarbilCK-1827452心肌肌球蛋白激動(dòng)劑重組人干擾素-α2bHuman IFN-a2b
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| 供貨周期 | 現(xiàn)貨 | 規(guī)格 | 5mg |
|---|---|---|---|
| 貨號(hào) | S2623 | 主要用途 | 科研 |
Omecamtiv mecarbil (CK-1827452)/心肌肌球蛋白激動(dòng)劑
Omecamtiv mecarbil (CK-1827452)是一種特異性的心肌肌球蛋白激動(dòng)劑，是用于左心室收縮性心臟衰竭的臨床藥物。Phase 2。
化學(xué)數(shù)據(jù)
| 分子量 | 401.43 | 穩(wěn)定性 | 3年 -20°C粉狀 |
|---|---|---|---|
| 化學(xué)式 | C20H24FN5O3 | -- -- -- | |
| CAS號(hào) | 873697-71-3 | 別名 | N/A |
| Solubility (25°C) * | 體外 | DMSO | 80 mg/mL (199.28 mM) |
| Ethanol | 6 mg/mL (14.94 mM) | ||
| Water | Insoluble | ||
| 體內(nèi) | 1% DMSO+30% polyethylene glycol+1% Tween 80 | 30 mg/mL | |
| * <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. | |||
| 化學(xué)名 | methyl 4-(2-fluoro-3-(3-(6-methylpyridin-3-yl)ureido)benzyl)piperazine-1-carboxylate | ||
制備儲(chǔ)備液
| 濃度溶劑體積(DMSO)質(zhì)量 | 1 mg | 5 mg | 10 mg |
| 1 mM | 2.4911 mL | 12.4555 mL | 24.9109 mL |
| 5 mM | 0.4982 mL | 2.4911 mL | 4.9822 mL |
| 10 mM | 0.2491 mL | 1.2455 mL | 2.4911 mL |
| 50 mM | 0.0498 mL | 0.2491 mL | 0.4982 mL |
生物活性
| 產(chǎn)品描述 | Omecamtiv mecarbil (CK-1827452)是一種特異性的心肌肌球蛋白激動(dòng)劑，是用于左心室收縮性心臟衰竭的臨床藥物。Phase 2。 | |||||
|---|---|---|---|---|---|---|
| 靶點(diǎn) |
| |||||
| 體外研究 | 在體外，Omecamtiv mecarbil通過(guò)增加肌球蛋白ATPase比率，選擇性激活心肌肌球蛋白。 [1]在離體心肌細(xì)胞中，Omecamtiv mecarbil導(dǎo)致肌細(xì)胞收縮性增加，并使肌漿球蛋白抑制劑BDM失效，而不增加鈣轉(zhuǎn)運(yùn)或抑制PDE通路。[1] | |||||
| 體內(nèi)研究 | 在SD大鼠，深水動(dòng)物和心臟衰竭大鼠體內(nèi)，Omecamtiv mecarbil在血漿中濃度達(dá)到0.4 mM后顯著增加縮短分?jǐn)?shù)。[1]在清醒狀態(tài)下心肌梗死(MI-sHF)的狗體內(nèi)，Omecamtiv mecarbil顯著增加壁室厚度(25%)，每搏輸出量(44%)，心輸出量(22%)和左心室 (LV) 收縮射血時(shí)間(26%)。此外，Omecamtiv mecarbil也會(huì)導(dǎo)致一些血流動(dòng)力學(xué)參數(shù)，包括心率，平均左房壓，和LV末期舒張壓下降。在左心室肥大(LVH-sHF)的清醒的狗體內(nèi)，Omecamtiv mecarbil對(duì)血流動(dòng)力學(xué)參數(shù)具有類似且統(tǒng)計(jì)學(xué)差異化的影響。[2] | |||||
| 臨床實(shí)驗(yàn) | Omecamtiv mecarbil is currently in Phase II clinical trials in patients with Left Ventricular Systolic Dysfunction Hospitalized for Acute Heart Failure. | |||||
| 特征 | ||||||
*的實(shí)驗(yàn)操作 (此*來(lái)自于公開的文獻(xiàn)所以Selleck并不保證其有效性)
激酶實(shí)驗(yàn)：[1]
| 生化檢測(cè) | 心臟S1肌球蛋白和細(xì)絲蛋白(肌動(dòng)蛋白，肌鈣蛋白復(fù)合物，和原肌球蛋白)從牛心臟和兔子骨骼肌中制備。平滑肌肌球蛋白從雞胗中制備。ATPase試驗(yàn)以動(dòng)力學(xué)方式使用NADH耦合酶系統(tǒng)在pCa2+ = 6.75下進(jìn)行。比率標(biāo)準(zhǔn)化為DMSO對(duì)照組。 |
|---|
動(dòng)物實(shí)驗(yàn)：[1]
| 動(dòng)物模型 | Sprague Dawley 大鼠 |
|---|---|
| 配制 | Omecamtiv mecarbil在DMSO中溶解，然后在水中稀釋。 |
| 劑量 | ≤1.2 mg/kg/hour |
| 給藥處理 | i.v. |
參考
- [1] Anderson RL, et al. Mol Bio Cell, 2005, 16 (Abstract #1728).
- [2] Shen YT, et al. Circ Heart Fail. 2010, 3(4), 522-577.
客戶使用selleck產(chǎn)品的實(shí)驗(yàn)數(shù)據(jù)
數(shù)據(jù)來(lái)源于[Data independently produced by University of Illinois at Chicago, 2014]
Normal and Mutation human iPSC-CMs Structure when Treated with Omecamtiv Mecarbil. Human iPSC-CMs were plated on 100 kPa flat PDMS and grown for five days and left untreated, treated acuy on day 5, or treated continuously from the time of plating with the myosin activator Omecamtiv Mecarbil. iPSC-CMs were then fixed and stained for actin filaments (phalloidin, red) and nucleus (DAPI, blue). (a, c, e) Normal and (b, d, f) Mutation untreated, acuy treated, and continuously treated iPSC-CMs.
Omecamtiv mecarbil (CK-1827452)在6個(gè)文獻(xiàn)中得到引用
Myosin Activator Omecamtiv Mecarbil Increases Myocardial Oxygen Consumption and Impairs Cardiac Efficiency Mediated by Resting Myosin ATPase Activity [Bakkehaug JP, et al. Circ Heart Fail, 2015, 8(4):766-75]
PubMed: 26025342Molecular effects of the myosin activator omecamtiv mecarbil on contractile properties of skinned myocardium lacking cardiac myosin binding protein-C [Mamidi R, et al. J Mol Cell Cardiol, 2015, 85:262-272]
PubMed: 26100051Sarcomere length nanometry in rat neonatal cardiomyocytes expressed with α-actinin-AcGFP in Z discs. [Shintani SA, et al. J Gen Physiol, 2014, 143(4):513-24]
PubMed: 24638993Omecamtiv Mecarbil Modulates the Kinetic and Motile Properties of Porcine β-Cardiac Myosin. [Liu Y, et al. Biochemistry, 2015, 54(10):1963-75]
Bioengineering Approaches to Control Micromechanics for Analysis of Cardiomyocyte Contractility. [Broughton, et al. University of Illinois, 2014, Broughton]
Analytical Comparison of Natural and Pharmaceutical Ventricular Myosin Activators [Wang Y, et al. Biochemistry, 2014, 53(32):5298-306]
PubMed: 25068717
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Omecamtiv mecarbil (CK-1827452)/心肌肌球蛋白激動(dòng)劑
Omecamtiv mecarbil (CK-1827452)/心肌肌球蛋白激動(dòng)劑
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