Art. -Nr.: HY-12176

Aliskiren

(Synonyms: CGP 60536; CGP60536B; SPP 100)

11 Cited Publications

Kundenbewertung

Based on 11 publication(s) in Google Scholar

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

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Reinheit: 99.70%
CAS. Nr.: 173334-57-1
Formel: C₃₀H₅₃N₃O₆
Molecular Weight:551.76

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Aliskiren Chemical Structure

CAS. Nr.: 173334-57-1

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vivo
Chemical Information
Publications (11)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC50: 1.5 nM (renin)^[1]

In Vivo

Aliskiren (< 10 mg/kg, Orally, daily) inhibits plasma renin activity and lowers blood pressure in sodium-depleted marmosets^[2].
Aliskiren (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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 173334-57-1
Appearance Solid
Molecular Weight 551.76
Formel C₃₀H₅₃N₃O₆
Color White to light yellow
SMILES

COCCCOC1=CC(C[C@@H](C[C@@H]([C@H](C[C@H](C(NCC(C)(C(N)=O)C)=O)C(C)C)O)N)C(C)C)=CC=C1OC
Synonyms

CGP 60536; CGP60536B; SPP 100
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (11)

All WB

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Journal Impact Factor

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 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).
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

Prediction of drug-drug interaction risk of P-glycoprotein substrate in drug discovery. [Abstract]

2024 Jun:56:101008. PMID: 38663183
Stanford University

2025.
Toxicol Res Appl

2018, 2:239784731880115.
Toxicol Res Appl

September 25, 2018.
National Sun Yat-Sen University

2015 Sep.

Aliskiren 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.
East Tennessee State University

2015 May.

Lösungsmittel & Löslichkeit

In Vitro:

Ethanol : 100 mg/mL (181.24 mM; Need ultrasonic)

DMSO : 100 mg/mL (181.24 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.8124 mL

9.0619 mL

18.1238 mL

5 mM

0.3625 mL

1.8124 mL

3.6248 mL

10 mM

0.1812 mL

0.9062 mL

1.8124 mL

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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
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.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (4.53 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (4.53 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.53 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
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)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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 [Content Brief]

[2]. 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]

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

[4]. Chang AY, et al. Interplay between brain stem angiotensins and monocyte chemoattractant protein-1 as a novel mechanism for pressor response after ischemic stroke. Neurobiol Dis. 2014 Nov;71:292-304. [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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. 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
Ethanol / DMSO	1 mM	1.8124 mL	9.0619 mL	18.1238 mL	45.3096 mL
	5 mM	0.3625 mL	1.8124 mL	3.6248 mL	9.0619 mL
	10 mM	0.1812 mL	0.9062 mL	1.8124 mL	4.5310 mL
	15 mM	0.1208 mL	0.6041 mL	1.2083 mL	3.0206 mL
	20 mM	0.0906 mL	0.4531 mL	0.9062 mL	2.2655 mL
	25 mM	0.0725 mL	0.3625 mL	0.7250 mL	1.8124 mL
	30 mM	0.0604 mL	0.3021 mL	0.6041 mL	1.5103 mL
	40 mM	0.0453 mL	0.2265 mL	0.4531 mL	1.1327 mL
	50 mM	0.0362 mL	0.1812 mL	0.3625 mL	0.9062 mL
	60 mM	0.0302 mL	0.1510 mL	0.3021 mL	0.7552 mL
	80 mM	0.0227 mL	0.1133 mL	0.2265 mL	0.5664 mL
	100 mM	0.0181 mL	0.0906 mL	0.1812 mL	0.4531 mL

Aliskiren

11 Cited Publications

100 mg Angebot einholen

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Aliskiren

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Publications Citing Use of MedChemExpress (MCE) Aliskiren

Biologische Aktivität

Chemical Information

Publications (11)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Aliskiren

Anti-Infection Compound Library

Metabolism/Protease Compound Library

FDA-Approved Drug Library

Autophagy Compound Library

Drug Repurposing Compound Library

Anti-Cardiovascular Disease Compound Library

Anti-COVID-19 Compound Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Rare Diseases Drug Library

EMA-Approved Drug Library

FDA-Approved Anticancer Drug Library

Human Metabolite Library

Off-patent Drug Library

Antihypertensive Compound Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Nephrotoxicity Compound Library

Publications Citing Use of MedChemExpress (MCE) Aliskiren

Biologische Aktivität

Chemical Information

Publications (11)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Aliskiren Related Classifications

HY-12176 Related Classifications