Aliskiren Hemifumarate

Catalog No.S2199 Batch:S219904

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Technical Data

Formula

C30H53N3O6.1/2C4H4O4

Molecular Weight 609.83 CAS No. 173334-58-2
Solubility (25°C)* In vitro DMSO 100 mg/mL (163.98 mM)
Water 100 mg/mL (163.98 mM)
Ethanol 100 mg/mL (163.98 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.)

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Biological Activity

Description Aliskiren hemifumarate(CGP 60536 hemifumarate, CGP60536B hemifumarate, SPP 100 hemifumarate) is a direct renin inhibitor with IC50 of 1.5 nM.
Targets
Renin [1]
1.5 nM
In vitro

Aliskiren hemifumarate appears to bind to both the hydrophobic S1/S3-binding pocket and to a large, distinct subpocket that extends from the S3-binding site towards the hydrophobic core of renin. Oral bioavailability of Aliskiren hemifumarate is 2.4% in rats, 16% in marmosets and about 2.5% in humans. [2]

In vivo

Aliskiren hemifumarate (< 10 mg/kg, oral) inhibits plasma renin activity and lowers blood pressure in sodium-depleted marmosets. [3] Once-daily oral treatment with Aliskiren hemifumarate lowers blood pressure effectively, with a safety and tolerability profile, in patients with mild-to-moderate hypertension. [4]

Protocol (from reference)

Selleck's Aliskiren Hemifumarate has been cited by 2 publications

Aliskiren inhibits renin-mediated complement activation. [ Kidney Int, 2018, 94(4):689-700] PubMed: 29884545
Sympathoexcitation following intermittent hypoxia in rat is mediated by circulating angiotensin II acting at the carotid body and subfornical organ [ J Physiol, 2018, 596(15):3217-3232] PubMed: 29645283

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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.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.