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VTP-27999

Catalog No. T3064   CAS 942142-51-0
Synonyms: VTP27999

VTP-27999 is an alkyl amine Renin inhibitor. VTP-27999 has been used in trials studying the basic science of Renal Function.

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VTP-27999 Chemical Structure
VTP-27999, CAS 942142-51-0
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25 mg In stock $ 831.00
50 mg 4-6 weeks $ 1,080.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description VTP-27999 is an alkyl amine Renin inhibitor. VTP-27999 has been used in trials studying the basic science of Renal Function.
Kinase Assay PRMT3 biochemical assay: A radioactivity-based assay is optimized and used to determine the inhibition of PRMT3 in vitro. In a scintillation proximity assay (SPA), tritiated S-adenosylmethionine (3H-SAM) served as a methyl donor to methylate biotinylated histone peptide substrate. After completion of the reaction, the reaction mixture is transferred to the wells of a streptavidin / scintillant-coated microplate. The Biotinylated peptides binding to streptavidin coated resin, brings the incorporated 3H-methyl and the scintillant to close proximity. The amount of methylated peptide is quantified by tracing the radioactivity (counts per minute) as measured by the TopCount NXT? Microplate Scintillation and Luminescence Counter. Due to the very acidic nature of the 3H-SAM solution, non-tritiated (cold) SAM is used to supplement the reactions. The C-terminally biotinylated peptide composed of the first 24 amino acids residues of histone H4 (H4 1-24) is used as substrate. The typical assay mixture contained 0.01% Tween-20, 5 mM DTT, 20 nM PRMT3, 0.3 μM B-H4 1-24 and 28 μM (5 μM 3H-SAM plus 23 μM cold SAM) SAM in 20 mM Tris-HCl (pH 7.5) and a final volume of 20 μL. The IC50 values are determined at Km concentrations of both substrates by titration of the compound in the reaction mixture in a range between 2000-0.2 nM.
Synonyms VTP27999
Molecular Weight 525.08
Formula C26H41ClN4O5
CAS No. 942142-51-0

Storage

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

Solubility Information

DMSO: 10 mM

TargetMolReferences and Literature

1. Lanqi Jia et al. 2011, 2 (10), pp 747-751

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Keywords

VTP-27999 942142-51-0 Endocrinology/Hormones RAAS Inhibitor VTP27999 Renin VTP 27999 inhibit inhibitor

 

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