Aliskiren hemifumarate
Based on 11 publication(s) in Google Scholar
Aliskiren (CGP 60536; CGP60536B; SPP 100) hemifumarate is an orally active and selective renin inhibitor, with IC50 of 1.5 nM. Aliskiren hemifumarate can be used for the research of hypertension, cardiovascular diseases and cancer cachexia.
For research use only. We do not sell to patients.
- Purity: 99.62%
- CAS No.: 173334-58-2
- Formula: C64H110N6O16
- Molecular Weight:1219.59
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Aliskiren hemifumarate
More- Clin Sci. 2025 Jan 15;139(1):43-53. [Abstract]
- Biochem Pharmacol. 2025 Dec 13:245:117635. [Abstract]
- Neurobiol Dis. 2014 Nov;71:292-304. [Abstract]
- Lipids Health Dis. 2018 Jul 31;17(1):183. [Abstract]
- Front Biosci (Landmark Ed). 2023 Oct 17;28(10):238. [Abstract]
- Drug Metab Pharmacokinet. 2024 Jun:56:101008. [Abstract]
- Stanford University. 2025.
- Toxicol Res Appl. 2018, 2:239784731880115.
- Toxicol Res Appl. September 25, 2018.
- National Sun Yat-Sen University. 2015 Sep.
- East Tennessee State University. 2015 May.
Customer Validation & Images
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WB
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Biological Activity
IC50: 1.5 nM (renin)[1]; 0.6 nM (human renin), 2 nM (marmoset renin), 80 nM (rat renin), 7 nM (dog renin), 11 nM (rabbit renin), 63 nM (guinea pig renin), 150 nM (pig renin)[2]
Aliskiren hemifumarate inhibits plasma renin activity (PRA) in vitro with IC50s of 2.9 nM (human PRA), 8.0 nM (monkey PRA), respectively[1].
Aliskiren hemifumarate (5 μM; 24 h) inhibits prorenin-induced human aortic smooth muscle cell migration[2].
Aliskiren hemifumarate (1-10 μM; 24 h) inhibits both the lamellipodia formation and morphological changes induced by prorenin with no significant effect on PDGF-BB activity[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Smooth muscle cell (SMC)
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Concentration:1-10 μM
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Incubation Time:24 hours
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Result:Inhibited human aortic smooth muscle cell migration induced by prorenin (10 nM) at 10 μM.
Aliskiren hemifumarate (10 mg/kg; p.o.; single dose) delays cachexia development, reduces tumor, and prolongs mouse survival. And also improves whole‑body strength, mobility and coordination, enhances locomotor activity, and inhibits muscle wasting[4].
Aliskiren hemifumarate (10 mg/kg; p.o.; single dose; 20 d after C26 injection) reduces oxidative stress associated with cancer cachexia[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sodium-depleted marmosets[3]
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Dosage:3 mg/kg, 10 mg/kg
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Administration:Oral gavage; once daily; 12 days
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Result:Increased plasma immunoreactive renin levels, and lowered blood pressure without affecting heart rate.
Showed no rebound increase in BP following the end of treatment with either dose of aliskiren.
Inhibited the RAS and controls the upregulation of pro‑inflammatory cytokines.
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Animal Model:Cancer cachexia model in BALB/c mice injected with C26 mouse colon carcinoma cells[4]
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Dosage:10 mg/kg
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Administration:Oral gavage; on day 5 (as a preventive strategy, AP group) or on day 12 (as a therapeutic strategy, AT group) after C26 injection; for 20 days after C26 injection
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Result:Enhanced grip strength, coordination, and locomotor activity.
Inhibited serum Ang I and Ⅱ levels and both serum and muscular tumor necrosis factor‑α (TNF‑α) and inter‑ leukin‑6 (IL‑6) levels.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 173334-58-2
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Appearance Solid
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Molecular Weight 1219.59
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Formula C64H110N6O16
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Color White to off-white
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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
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Synonyms
CGP 60536 hemifumarate; CGP60536B hemifumarate; SPP 100 hemifumarate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (11)
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Journal Impact Factor
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Most Recent
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Clin Sci
Higher circulating ACE2 and DPP3 but reduced ACE and angiotensinogen in hyperreninemic sepsis patients. [Abstract]2025 Jan 15;139(1):43-53. PMID: 39699964 -
Biochem Pharmacol
Renin inhibition improved muscular function by alleviating insulin resistance and AGEs/RAGE signaling in skeletal muscle associated with high glucose: Exploration of renin inhibitor tanshinone IIA. [Abstract]2025 Dec 13:245:117635. PMID: 41391695 -
Neurobiol Dis
Interplay between brain stem angiotensins and monocyte chemoattractant protein-1 as a novel mechanism for pressor response after ischemic stroke. [Abstract]2014 Nov;71:292-304. PMID: 25131447 -
Lipids Health Dis
Combination of Chymostatin and Aliskiren attenuates ER stress induced by lipid overload in kidney tubular cells. [Abstract]2018 Jul 31;17(1):183. PMID: 30064425
Aliskiren hemifumarate purchased from MedChemExpress. Usage Cited in: Lipids Health Dis. 2018 Jul 31;17(1):183. [Abstract]
Protein abundance of ER stress markers (BiP, IRE1α, PERK, ATF4, pS51-eIF2α, eIF2α, and CHOP) are upregulated after palmitic acid (PA) treatment, which is prevented by cotreatment with chymostatin (50μM) and Aliskiren (10 nM).
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Front Biosci (Landmark Ed)
C3aR Antagonist Alleviates C3a Induced Tubular Profibrotic Phenotype Transition via Restoring PPARα/CPT-1α Mediated Mitochondrial Fatty Acid Oxidation in Renin-Dependent Hypertension. [Abstract]2023 Oct 17;28(10):238. PMID: 37919077 -
Drug Metab Pharmacokinet
2024 Jun:56:101008. PMID: 38663183 -
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Aliskiren hemifumarate purchased from MedChemExpress. Usage Cited in: National Sun Yat-Sen University. 2015 Sep.
Effects of Aliskiren (AK) produce efficacious antagonism of the protein expression of c-Fos (A), GFAP (B) and OX-42 (C) in SC, aCSF+MCAO, AK+MCAO or AK alone group one day after stroke.
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Solvent & Solubility
H2O : ≥ 50 mg/mL (41.00 mM)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 50 mg/mL (41.00 mM); Clear solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Purity & Documentation
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Data Sheet (280 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[2]. Ferri N, et al. Aliskiren inhibits prorenin-induced human aortic smooth muscle cell migration. J Renin Angiotensin Aldosterone Syst. 2015 Jun;16(2):284-91. [Content Brief]
[3]. Wood JM, et al. Structure-based design of aliskiren, a novel orally effective renin inhibitor.Biochem Biophys Res Commun, 2003, 308(4), 698-705. [Content Brief]
[4]. Wang C, et al. Aliskiren targets multiple systems to alleviate cancer cachexia. Oncol Rep. 2016 Nov;36(5):3014-3022. [Content Brief]
[5]. Buczko W, et al. Pharmacokinetics and pharmacodynamics of aliskiren, an oral direct renin inhibitor. Pharmacol Rep. 2008 Sep-Oct;60(5):623-31. [Content Brief]
[6]. Gradman AH, et al.Aliskiren, a novel orally effective renin inhibitor, provides dose-dependent antihypertensive efficacy and placebo-like tolerability in hypertensive patients. Circulation, 2005, 111(8), 1012-1018. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 0.8199 mL | 4.0997 mL | 8.1995 mL | 20.4987 mL |
| 5 mM | 0.1640 mL | 0.8199 mL | 1.6399 mL | 4.0997 mL | |
| 10 mM | 0.0820 mL | 0.4100 mL | 0.8199 mL | 2.0499 mL | |
| 15 mM | 0.0547 mL | 0.2733 mL | 0.5466 mL | 1.3666 mL | |
| 20 mM | 0.0410 mL | 0.2050 mL | 0.4100 mL | 1.0249 mL | |
| 25 mM | 0.0328 mL | 0.1640 mL | 0.3280 mL | 0.8199 mL | |
| 30 mM | 0.0273 mL | 0.1367 mL | 0.2733 mL | 0.6833 mL | |
| 40 mM | 0.0205 mL | 0.1025 mL | 0.2050 mL | 0.5125 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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