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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, CAS 442908-10-3

Pack Size	Availability	Price/USD
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%

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	A1:69 nM(Ki), A2A:1.3 nM(Ki)
In vivo	Vipadenant, administered at doses ranging from 0.3 to 30 mg/kg, effectively reduces catalepsy in a dose-dependent manner without inducing statistically significant dyskinetic episodes in 6-OHDA-lesioned rats at a dosage of 10 mg/kg through a 19-day treatment protocol. Moreover, in models of haloperidol-induced hypolocomotion in mice and rats, the minimum effective doses of vipadenant are 0.1 mg/kg and 1 mg/kg, respectively. Additionally, oral administration of vipadenant at 3 and 10 mg/kg is shown to increase contralateral rotations in 6-OHDA lesioned rats, indicating its potential in modulating motor functions.
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

References 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 Active Compound Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Membrane Protein-targeted Compound Library Drug Repurposing Compound Library GPCR Compound Library Inhibitor Library Anti-Neurodegenerative Disease Compound Library Immuno-Oncology Compound Library Anti-Obesity 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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