Aliskiren fumarate(Synonyms: CGP 60536 fumarate; CGP60536B fumarate; SPP 100 fumarate)

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Aliskiren fumarate (Synonyms: CGP 60536 fumarate; CGP60536B fumarate; SPP 100 fumarate)

Aliskiren fumarate 是一种口服有效的、选择性的肾素 (renin) 抑制剂，其 IC50 为 1.5 nM。Aliskiren fumarate 可用于高血压、心血管疾病和癌症恶病质的研究。

Aliskiren fumarate(Synonyms: CGP 60536 fumarate; CGP60536B fumarate; SPP 100 fumarate)

Aliskiren fumarate Chemical Structure

CAS No. : 1196835-68-3

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Aliskiren fumarate 的其他形式现货产品:

Aliskiren

生物活性

Aliskiren fumarate is an orally active, highly potent and selective renin inhibitor, with IC50 of 1.5 nM. Aliskiren fumarate can be used for the research of hypertension, cardiovascular diseases and cancer cachexia[1][2][3].

IC50 & Target

IC50: 1.5 nM (renin)[1]
体内研究
(In Vivo)

Aliskiren fumarate (< 10 mg/kg, Orally, daily) inhibits plasma renin activity and lowers blood pressure in sodium-depleted marmosets[2].
Aliskiren fumarate (10 mg/kg, Intragastrically, once) significantly alleviates multiple cachexia‑associated symptoms in BALB/c mice bearing C26 mouse colon carcinoma cells, including BW loss, tumor burden, muscle wasting, muscular dysfunction, and shortened survival[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

667.83

Formula

C34H57N3O10
CAS 号

1196835-68-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Yuji Nakamura, et al. Discovery of DS-8108b, a Novel Orally Bioavailable Renin Inhibitor. ACS Med. Chem. Lett., 2012, 3 (9), pp 754–758

    [2]. Wood JM, et al. Structure-based design of aliskiren, a novel orally effective renin inhibitor. Biochem Biophys Res Commun. 2003 Sep 5;308(4):698-705.

    [3]. Wang C, et al. Aliskiren targets multiple systems to alleviate cancer cachexia. Oncol Rep. 2016 Nov;36(5):3014-3022.

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