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Vipadenant

Catalog No. T2373   CAS 442908-10-3
Synonyms: CEB-4520, BIIB-014

Vipadenant (CEB-4520)(BIIB-014) is an adenosine A2a antagonist with Ki of 1.3 nM; less potent for A1(Ki=69 nM).

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Vipadenant Chemical Structure
Vipadenant, CAS 442908-10-3
Pack Size Availability Price/USD Quantity
1 mg In stock $ 34.00
2 mg In stock $ 48.00
5 mg In stock $ 79.00
10 mg In stock $ 122.00
25 mg In stock $ 222.00
50 mg In stock $ 369.00
100 mg In stock $ 549.00
500 mg In stock $ 1,190.00
1 mL * 10 mM (in DMSO) In stock $ 378.00
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Purity: 98%
Purity: 97.25%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Vipadenant (CEB-4520)(BIIB-014) is an adenosine A2a antagonist with Ki of 1.3 nM; less potent for A1(Ki=69 nM).
Targets&IC50 adenosine A1:69 nM(Ki), adenosine A2a:1.3 nM(Ki)
In vivo Vipadenant (0.3-30 mg/kg) produces a reduction in catalepsy in a dose-dependent manner. Vipadenant (10 mg/kg) does not produce any statistically significant dyskinetic episodes in 6-OHDA-lesioned rats during a 19-day dosing regimen[1]. In the mouse and rat haloperidol-induced hypolocomotion models, vipadenant has a minimum effective dose of 0.1 and 1 mg/kg, respectively. Vipadenant (3 and 10 mg/kg, p.o.) can increase contralateral rotations in 6-OHDA lesioned rats[2].
Kinase Assay Peptide substrate phosphorylation assays with GST-Abl kinase domains: The effect of AP24534 (0-320 nM) on GST-Abl kinase activity is assessed by using a synthetic peptide substrate (Abltide: EAIYAAPFAKKK). Assays are carried out at 30 °C for 15 min in 25 μL reaction mixture: 8 mM MOPS (pH 7), 0.2 mM EDTA, 50 μM Abltide, 30 mM MgCl2, 10 mM β-glycerol phosphate, 1 mM EGTA, 0.002% Brij-35, 0.4 mM DTT, 0.2 mg/mL BSA, 0.4 mM sodium orthovanadate, 10 nM WT or mutant GST-Abl kinase, and 100 μM ATP/γ-32[P]ATP (5000 cpm/pmol). Reactions are terminated by transferring a portion of the reaction mixture onto a p81 phosphocellulose filter and immersing in 0.75% phosphoric acid. Filters are washed 3 times in 0.75% phosphoric acid, rinsed in acetone, and air dried; phosphate incorporation is determined by scintillation counting. All results are corrected for background binding to the filters, as determined by omitting peptide substrate from the kinase reaction. Time course experiments to establish the linear range of enzymatic activity precedes kinase assays.
Synonyms CEB-4520, BIIB-014
Molecular Weight 321.34
Formula C16H15N7O
CAS No. 442908-10-3

Storage

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

Solubility Information

DMSO: 31 mg/mL

TargetMolReferences and Literature

1. Jones N, et al. A2A receptor antagonists do not induce dyskinesias in drug-naive or L-dopa sensitized rats. Brain Res Bull. 2013 Sep;98:163-9. 2. Shook B C , Jackson P F . Adenosine A2A Receptor Antagonists and Parkinson’s Disease[J]. ACS Chemical Neuroscience, 2011, 2(10):555-567.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Anti-Cancer Active Compound Library Anti-Neurodegenerative Disease Compound Library Bioactive Compound Library Neurotransmitter Receptor Compound Library Preclinical Compound Library GPCR Compound Library Neuronal Signaling Compound Library Anti-Cancer Compound Library

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Keywords

Vipadenant 442908-10-3 GPCR/G Protein Neuroscience Adenosine Receptor CEB4520 BIIB 014 BIIB014 inhibit CEB 4520 Inhibitor P1 receptor CEB-4520 BIIB-014 inhibitor

 

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