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Aliskiren Hemifumarate RAAS inhibitor

Name: Aliskiren Hemifumarate
Brand: Selleck Chemicals
SKU: S2199
Availability: InStock
Rating: 5 (3 reviews)

Cat.No.S2199

Aliskiren hemifumarate(CGP 60536 hemifumarate, CGP60536B hemifumarate, SPP 100 hemifumarate) is a direct renin inhibitor with IC50 of 1.5 nM.

Chemical Structure

Molecular Weight: 609.83

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.97%

99.97

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Chemical Information, Storage & Stability

Molecular Weight	609.83	Formula	C₃₀H₅₃N₃O₆.1/2C₄H₄O₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	173334-58-2	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	CGP 60536 hemifumarate, CGP60536B hemifumarate, SPP 100 hemifumarate			Smiles	CC(C)C(CC1=CC(=C(C=C1)OC)OCCCOC)CC(C(CC(C(C)C)C(=O)NCC(C)(C)C(=O)N)O)N.CC(C)C(CC1=CC(=C(C=C1)OC)OCCCOC)CC(C(CC(C(C)C)C(=O)NCC(C)(C)C(=O)N)O)N.C(=CC(=O)O)C(=O)O

Solubility

In vitro
Batch:

DMSO : 122 mg/mL (200.05 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 122 mg/mL

Ethanol : 122 mg/mL

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	Renin ^[1] 1.5 nM
In vitro	Aliskiren hemifumarate appears to bind to both the hydrophobic S1/S3-binding pocket and to a large, distinct subpocket that extends from the S3-binding site towards the hydrophobic core of renin. Oral bioavailability of Aliskiren hemifumarate is 2.4% in rats, 16% in marmosets and about 2.5% in humans. ^[2]
In vivo	Aliskiren hemifumarate (< 10 mg/kg, oral) inhibits plasma renin activity and lowers blood pressure in sodium-depleted marmosets. ^[3] Once-daily oral treatment with Aliskiren hemifumarate lowers blood pressure effectively, with a safety and tolerability profile, in patients with mild-to-moderate hypertension. ^[4]
References	[1] http://pubs.acs.org/doi/full/10.1021/ml300168e [2] https://pubmed.ncbi.nlm.nih.gov/19066408/ [3] https://pubmed.ncbi.nlm.nih.gov/12927775/ [4] https://pubmed.ncbi.nlm.nih.gov/15723979/ [5] https://pubmed.ncbi.nlm.nih.gov/17658393/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04432350	Withdrawn	COVID\|Drug Effect\|Drug Interaction\|Risk Reduction	Tabula Rasa HealthCare	June 12 2020	--
NCT01570686	Completed	Hypertension	Novartis Pharmaceuticals\|Novartis	April 2012	Phase 4
NCT01519635	Completed	Hypertension	Centre Hospitalier Universitaire Vaudois	October 2011	Phase 4
NCT01235910	Terminated	Hypertension\|Cardiac Transplantation	University of Colorado Denver\|American Heart Association	May 2011	Phase 4

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