Home Tools
Log in
Cart

Aliskiren hemifumarate

Catalog No. T1520   CAS 173334-58-2
Synonyms: CGP 60536, SPP 100, CGP60536B

Aliskiren hemifumarate (CGP60536B) is an orally active nonpeptide renin inhibitor with antihypertensive activity.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Aliskiren hemifumarate Chemical Structure
Aliskiren hemifumarate, CAS 173334-58-2
Pack Size Availability Price/USD Quantity
5 mg In stock $ 34.00
10 mg In stock $ 50.00
25 mg In stock $ 55.00
50 mg In stock $ 98.00
100 mg In stock $ 164.00
200 mg In stock $ 297.00
1 mL * 10 mM (in DMSO) In stock $ 62.00
Bulk Inquiry
Get quote
Select Batch  
Purity: 99.7%
Purity: 99%
Purity: 96.18%
Contact us for more batch information
Biological Description
Chemical Properties
Storage & Solubility Information
Description Aliskiren hemifumarate (CGP60536B) is an orally active nonpeptide renin inhibitor with antihypertensive activity.
Targets&IC50 Renin: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]
Kinase Assay Radioligand Binding Assay: Human CB1 and CB2 stably transfect HEK 293 cells and cell membrane is purified. 0.2-8 μg of the purified membrane is incubated with 0.75 nM [3H] CP55,940 and Rimonabant in the incubation buffer (50 mM Tris-HCl, 5 mM MgCl2, 1 mM EDTA, 0.3%BSA, pH 7.4). The non-specific binding is defined in the presence of 1 μM of CP55,940. The reactions are incubated for one and a half hours at 30 °C in Multiscreen. The reactions are terminated by manifold filtration and washed four times with ice-cold wash buffer (50 mM Tris, pH 7.4, 0.25% BSA).The radioactivity bound to the filters is measured by Topcount. The IC50 is determined as the concentration of Rimonabant required to inhibit 50% of the binding of [3H] CP55,940 and calculated by non-linear regression.
Synonyms CGP 60536, SPP 100, CGP60536B
Molecular Weight 1219.6
Formula C30H53N3O6·1/2C4H4O4
CAS No. 173334-58-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 93 mg/mL (76.3 mM)

H2O: 92 mg/mL (75.4 mM)

Ethanol: 93 mg/mL (76.3 mM)

TargetMolReferences and Literature

1. Nakamura Y, et al. ACS Med Chem Lett, 2012, 3(9), 754–758. 2. Buczko W, et al. Pharmacol Rep, 2008, 60(5), 623-631. 3. Wood JM, et al. Biochem Biophys Res Commun, 2003, 308(4), 698-705. 4. Gradman AH, et al. Circulation, 2005, 111(8), 12012-12018. 5. Oparil S, et al. Lancet, 2007, 370(9583), 221-229.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Approved Drug Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Approved Drug Library Inhibitor Library Clinical Compound Library Endocrinology-Hormone Compound Library Anti-Metabolism Disease Compound Library Bioactive Compounds Library Max Drug-induced Liver Injury (DILI) Compound Library

Related Products

Related compounds with same targets
KJ Pyr 9 Naringin AS1842856 Gimeracil Etoposide Quinacrine dihydrochloride Linagliptin Clinofibrate

TargetMolDose Conversion

You can also refer to dose conversion for different animals. More

TargetMol In vivo Formulation Calculator (Clear solution)

Step One: Enter information below
Dosage
mg/kg
Average weight of animals
g
Dosing volume per animal
ul
Number of animals
Step Two: Enter the in vivo formulation
% DMSO
%
% Tween 80
% ddH2O
Calculate Reset

TargetMolCalculator

Molarity Calculator
Dilution Calculator
Reconstitution Calculation
Molecular Weight Calculator
=
X
X

Molarity Calculator allows you to calculate the

  • Mass of a compound required to prepare a solution of known volume and concentration
  • Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Concentration of a solution resulting from a known mass of compound in a specific volume
See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

X
=
X

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

=
/

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Aliskiren hemifumarate 173334-58-2 Autophagy Endocrinology/Hormones RAAS Aliskiren SPP 100 hemifumarate CGP60536B hemifumarate cardiovascular diseases SPP-100 colon carcinoma cachexia cancer CGP 60536 hemifumarate Aliskiren Hemifumarate CGP 60536 Renin inhibit Hypertension C26 SPP 100 SPP100 CGP60536B CGP60536 CGP-60536 Inhibitor inhibitor

 

TargetMol