Omecamtiv mecarbil (CK-1827452) 化学構造
分子量: 401.43

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製品説明

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製品の説明

生物活性

製品説明 Omecamtivmecarbil(CK-1827452)は、特定の心臓ミオシン活性剤と左室収縮期の心臓麻痺のための臨床薬です。
ターゲット
IC50
In vitro試験 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試験 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]
臨床試験 Omecamtiv mecarbil is currently in Phase II clinical trials in patients with Left Ventricular Systolic Dysfunction Hospitalized for Acute Heart Failure.
特集

プロトコル (参考用のみ)

キナーゼアッセイ: [1]

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: [1]

動物モデル Sprague Dawley rats.
製剤 Omecamtiv mecarbil is dissolved in DMSO and then diluted in water.
投薬量 ≤1.2 mg/kg/hour
投与方法 Administered via i.v.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download Omecamtiv mecarbil (CK-1827452) SDF
分子量 401.43
化学式

C20H24FN5O3

CAS No. 873697-71-3
保管 2年-20℃
6月-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 80 mg/mL (199.28 mM)
エタノール 6 mg/mL (14.94 mM)
<1 mg/mL (<1 mM)
In vivo 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.
化学名 methyl 4-(2-fluoro-3-(3-(6-methylpyridin-3-yl)ureido)benzyl)piperazine-1-carboxylate

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Source University of Illinois at Chicago, 2014, Omecamtiv mecarbil (CK-1827452) purchased from Selleck
Method Immunofluorescence
Cell Lines iPSC-CM cells
Concentrations
Incubation Time 5 days
Results Phalloidin immunohistochemistry of the untreated, acutely treated and continuously treated with Omecamtiv Mecarbil normal and mutation iPSC-CM cells show F-actin structure.

文献中の引用 (4)

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description
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