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Aliskiren hemifumarate

Cat. No. 5491 Submit a Review Datasheet / COA / SDS
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Description: Potent renin inhibitor; antihypertensive
Alternative Names: SPP 100
Chemical Name: (αS,γS,δS,ζS)-δ-Amino-N-(3-amino-2,2-dimethyl-3-oxopropyl)-γ-hydroxy-4-methoxy-3-(3-methoxypropoxy)-α,ζ-bis(1-methylethyl)benzeneoctanamide hemifumarate
Purity: ≥99% (HPLC)
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Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for Aliskiren hemifumarate

Aliskiren hemifumarate is a potent renin inhibitor (IC50 = 0.6 and 80 nM for human and rat respectively). Exhibits selectivity for renin over a range of other aspartic proteinases (>5000 nM). Lowers blood pressure in a hypertensive rodent model. Orally active.

Compound Libraries for Aliskiren hemifumarate

Aliskiren hemifumarate is also offered as part of the Tocriscreen FDA-Approved Drugs. Find out more about compound libraries available from Tocris.

Technical Data for Aliskiren hemifumarate

M. Wt 609.83
Formula C30H53N3O6.1/2C4H4O4
Storage Store at -20°C
Purity ≥99% (HPLC)
CAS Number 173334-58-2
PubChem ID 6918427
InChI Key KLRSDBSKUSSCGU-KRQUFFFQSA-N
Smiles COC1=C(OCCCOC)C=C(C[C@H]([C@@H](C)C)C[C@@H]([C@@H](O)C[C@@H]([C@@H](C)C)C(NCC(C)(C)C(N)=O)=O)N)C=C1.COC2=C(OCCCOC)C=C(C[C@H]([C@@H](C)C)C[C@@H]([C@@H](O)C[C@@H]([C@@H](C)C)C(NCC(C)(C)C(N)=O)=O)N)C=C2.O=C(/C=C/C(O)=O)O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for Aliskiren hemifumarate

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
water 60.98 100
DMSO 60.98 100

Preparing Stock Solutions for Aliskiren hemifumarate

The following data is based on the product molecular weight 609.83. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.64 mL 8.2 mL 16.4 mL
5 mM 0.33 mL 1.64 mL 3.28 mL
10 mM 0.16 mL 0.82 mL 1.64 mL
50 mM 0.03 mL 0.16 mL 0.33 mL

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Product Datasheets for Aliskiren hemifumarate

Certificate of Analysis / Product Datasheet
Safety Datasheet

References for Aliskiren hemifumarate

References are publications that support the biological activity of the product.

Jensen et al (2) Aliskiren: the first renin inhibitor for clinical treatment. Nat.Rev.Drug Discov. 7 399 PMID: 18340340

Kaye and Krum (2007) Drug discovery for heart failure: a new era or the end of the pipeline? Nat.Rev.Drug Discov. 6 127 PMID: 17268484

If you know of a relevant reference for Aliskiren hemifumarate, please let us know.

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Citations for Aliskiren hemifumarate

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