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Aliskiren hemifumarate

Name: Aliskiren hemifumarate
Brand: TargetMol
SKU: T1520
Price: 34 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T1520Cas No. 173334-58-2

Alias SPP 100, CGP60536B, CGP 60536

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

Aliskiren hemifumarate

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Purity: 99.21%

Catalog No. T1520Alias SPP 100, CGP60536B, CGP 60536Cas No. 173334-58-2

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

Pack Size	Price	USA Warehouse	Global Warehouse
5 mg	$34	In Stock	In Stock
10 mg	$50	In Stock	In Stock
25 mg	$55	In Stock	In Stock
50 mg	$98	In Stock	In Stock
100 mg	$164	In Stock	In Stock
200 mg	$297	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$62	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Purity:99.21%

Color:White

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COA HNMR LCMS

Product Introduction

Bioactivity

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	SPP 100, CGP60536B, CGP 60536

Chemical Properties

Molecular Weight	1219.6
Formula	C₃₀H₅₃N₃O₆·1/2C₄H₄O₄
Cas No.	173334-58-2
Smiles	C(=O)(/C=C/C(=O)O)O.C(=O)([C@@H](C[C@@H]([C@H](C[C@@H](C(C)C)Cc1cc(c(cc1)OC)OCCCOC)N)O)C(C)C)NCC(C(=O)N)(C)C.C(=O)([C@@H](C[C@@H]([C@H](C[C@@H](C(C)C)Cc1cc(c(cc1)OC)OCCCOC)N)O)C(C)C)NCC(C(=O)N)(C)C
Relative Density.	no data available

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 93 mg/mL (76.25 mM), Sonication is recommended.

H2O: 92 mg/mL (75.43 mM), Sonication is recommended.

Ethanol: 93 mg/mL (76.25 mM), Sonication is recommended.

Solution Preparation Table

H2O/DMSO/Ethanol

	1mg	5mg	10mg	50mg
1 mM	0.8199 mL	4.0997 mL	8.1994 mL	40.9970 mL
5 mM	0.1640 mL	0.8199 mL	1.6399 mL	8.1994 mL
10 mM	0.0820 mL	0.4100 mL	0.8199 mL	4.0997 mL
20 mM	0.0410 mL	0.2050 mL	0.4100 mL	2.0499 mL
50 mM	0.0164 mL	0.0820 mL	0.1640 mL	0.8199 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

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

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