Aliskiren hemifumarate

Pricing Availability Delivery Time Qty
Cat.No. 5491 - Aliskiren hemifumarate | C30H53N3O6.1/2C4H4O4 | CAS No. 173334-58-2
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)
Datasheet
Citations
Literature

Biological Activity

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

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

Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Preparing Stock Solutions

The following data is based on the product molecular weight 609.83. Batch specific molecular weights may vary from batch to batch due to solvent 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

Safety Datasheet

References

References are publications that support the products' biological activity.

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


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Keywords: SPP100 Potent renin inhibitors inhibits hypertensive hypertension blood pressure heart SPP 100 Other Proteases

Citations for Aliskiren hemifumarate

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