Aliskiren Hemifumarate

製品コードS2199 バッチS219904

印刷

化学情報

Chemical Structure Synonyms CGP 60536 hemifumarate, CGP60536B hemifumarate, SPP 100 hemifumarate Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C30H53N3O6.1/2C4H4O4
分子量 609.83 CAS No. 173334-58-2
Solubility (25°C)* 体外 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Aliskiren hemifumarate(CGP 60536 hemifumarate, CGP60536B hemifumarate, SPP 100 hemifumarate) is a direct renin inhibitor with IC50 of 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]

プロトコル(参考用のみ)

キナーゼアッセイ Enzyme inhibition assay
All reactions are carried out in a flat bottom black opaque microtiter plate. Aliskiren hemifumarate in DMSO (2 μL) are mixed with 100 μL of the assay buffer (50 mM Tris-HCl (pH7.9), 100 mM NaCl) containing 5 μL of trypsin-activated recombinant human renin (final enzyme concentration of 50 μM), and the solution is pre-incubated at room temperature for 10 min. Next, 2 μM of the substrate (Arg-Glu(EDANS)-Ile-His-Pro-Phe-His-Leu-Val-Ile-His-Thr-Lys(DABCYL)-Arg) in 100 μL of the assay buffer is added, and the resulting mixture is incubated at 37 °C for 90 min. After completion of incubation, the concentration of generated angiotensin I is measured by fluorescence at 492 nm (excitation at 340 nm) using a multilabel reader.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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

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。