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My CartCAS：173334-58-2
Storage：Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to off-white Solid
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| CAS | 173334-58-2 |
| Name | Aliskiren Hemifumarate |
| Molecular Formula | C30H53N3O6·1/2C4H4O4 |
| Molecular Weight | 609.79 |
| Solubility | Soluble in Water/DMSO |
| Purity | ≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC | EINECS 630-415-8 |
| MDL | MFCD10566724 |
| SMILES | O=C(O)/C=C/C(O)=O.O=C(NCC(C)(C(N)=O)C)[C@@H](C[C@@H]([C@H](C[C@@H](C(C)C)CC1=CC=C(OC)C(OCCCOC)=C1)N)O)C(C)C.O=C(NCC(C)(C(N)=O)C)[C@H](C(C)C)C[C@H](O)[C@@H](N)C[C@@H](C(C)C)CC2=CC=C(OC)C(OCCCOC)=C2 |
| Target Point | Renin |
| Passage | Endocrinology & Hormones |
| Background | It is a direct inhibitor of renin. |
| Biological Activity | Aliskiren Hemifumarate是一种直接肾素抑制剂，IC50为1.5 nM。[1] |
| In Vitro | Aliskiren hemifumarate似乎会结合到疏水性S1/S3-结合口袋和从S3-结合位点延伸到肾素疏水核的大的，明显的亚口袋。Aliskiren hemifumarate的口服利用度在大鼠，狨猴和人类中分别为2.4%，16%和2.5%。[2] |
| In Vivo | 在钠耗竭的狨猴体内，Aliskiren hemifumarate(< 10 mg/kg，口服)抑制血浆肾素活性，并降低血压。[3]在轻度至中度高血压患者中，Aliskiren hemifumarate每天一次口服治疗有效降低血压，并且具有安全性和耐受性。[4] |
| Data Literature Source | [1] Nakamura Y，et al. ACS Med Chem Lett，2012，3(9)，754–758. [2] Buczko W，et al. Pharmacol Rep，2008，60(5)，623-631. [3] Wood JM，et al. Biochem Biophys Res Commun，2003，308(4)，698-705. [4] Gradman AH，et al. Circulation，2005，111(8)，1012-1018. |
| Unit | Bottle |
| Specification | 25mg 50mg |
是肾素的直接抑制剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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