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Formula | C30H53N3O6 |
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Molecular Weight | 551.76 | CAS No. | 173334-57-1 | |
Solubility (25°C)* | In vitro | DMSO | 100 mg/mL (181.23 mM) | |
Ethanol | 100 mg/mL (181.23 mM) | |||
Water | 6 mg/mL (10.87 mM) | |||
* <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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | Aliskiren(CGP 60536) is a renin inhibitor with antihypertensive activity. | |
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In vitro | Aliskiren is the fourth class of pharmacological agents that modify the function of RAAS. It is an octanamide, is the first known representative of a new class of completely nonpeptide, low-molecular-weight, orally active transition-state renin inhibitors. Aliskiren has good water solubility and low lipophilicity, and is resistant to biodegradation by peptidases in the intestine, blood circulation, and the liver. Aliskiren has 10,000-fold higher affinity for renin than for other aspartic peptidases[1]. |
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In vivo | In short-term studies, Aliskiren is effective in lowering blood pressure either alone or in combination with valsartan and hydrochlorothiazide, and had a low incidence of serious adverse effects. Aliskiren has a half-life of approximately 40 h, making it suitable for once-daily dosing, with less potential for loss of efficacy between doses than shorter acting agents. Aliskiren exhibits oral bioavailability due to its low molecular weight (609.8 Da) and nonpeptide structure, making it more resistant to gastrointestinal enzyme disintegration. However, it is still poorly absorbed (oral bioavailability, ∼2.5%). Aliskiren is 50% protein bound, and the apparent volume of distribution is 135 L. Aliskiren is slightly metabolized in humans (about 20%) and is approximately 50% metabolized in rodents. Aliskiren effectively reduces functional plasma renin activity by binding to renin with high affinity, preventing it from converting angiotensinogen to angiotensin I. The inhibition of renin by aliskiren is associated with a reduction in circulating levels of angiotensin I and II, with a resultant increase in plasma renin concentration and inhibit activation of mitogen-activated protein kinases ERK1 (p44) and ERK2 (p42). It prevents hypertrophy and proliferation. Aliskiren is well tolerated, with the most common adverse events reported as headache, dizziness, and fatigue[1]. |
Aliskiren decreases oxidative stress and angiogenic markers in retinal pigment epithelium cells. [ Angiogenesis, 2017, 20(1):175-181] | PubMed: 27695972 |
Local renin-angiotensin system mediates endothelial dilator dysfunction in aging arteries. [ Am J Physiol Heart Circ Physiol, 2016, 311(3):H849-54] | PubMed: 27422988 |
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
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