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ST-1535

Catalog No. T28861 CAS 496955-42-1

ST 1535 is a potent and orally active antagonist of A2A adenosine receptor with antiparkinsonian activity and antitremorigenic effects. ST 1535 exhibits the potential for the research of Parkinson’s disease.

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ST-1535, CAS 496955-42-1

Pack Size	Availability	Price/USD
1 mg	In stock	$ 67.00
5 mg	In stock	$ 143.00
10 mg	In stock	$ 195.00
25 mg	In stock	$ 340.00
50 mg	In stock	$ 493.00
100 mg	In stock	$ 719.00
1 mL * 10 mM (in DMSO)	In stock	$ 148.00

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Purity: 99.64%

Purity: 99.63%

Biological Description

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Description	ST 1535 is a potent and orally active antagonist of A2A adenosine receptor with antiparkinsonian activity and antitremorigenic effects. ST 1535 exhibits the potential for the research of Parkinson’s disease.
In vitro	ST-1535 competitively antagonizes the effects of the A2A adenosine agonist NECA on cAMP in cells cloned with the human A2A adenosine receptor (IC50=353+/-30 nM), and the effects of the A1 adenosine agonist CHA on cAMP in cells cloned with the human A1 adenosine receptor (IC50=510+/-38 nM). [1]
In vivo	ST 1535, at oral doses of 5 and 10 mg/kg, antagonizes catalepsy induced by intracerebroventricular administration of the A2A adenosine agonist CGS 21680 (10 microg/5 microl) in mice. At oral doses ranging between 5 and 20 mg/kg, ST 1535 induces hypermotility and antagonizes haloperidol-induced catalepsy in mice up to 7 h. Oral ST 1535, at 1.25 and 2.5 mg/kg, potentiates L-dopa effects in reducing haloperidol-induced catalepsy. [1]

Molecular Weight	272.31
Formula	C12H16N8
CAS No.	496955-42-1

Storage

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

Solubility Information

DMSO: 9 mg/mL (33.05 mM)

References and Literature

1. Maria Antonietta Stasi, et al. ST 1535: a preferential A2Aadenosinereceptor antagonist. Int J Neuropsychopharmacol. 2006 Oct;9(5):575-84. 2. Giovanni Piersanti, et al. Synthesis and biological evaluation of metabolites of 2-n-butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine (ST1535), a potent antagonist of the A2A adenosine receptor for the treatment of Parkinson's disease. J Med Chem. 2013 Jul 11;56(13):5456-63. 3. Lucia Frau, et al. Neuroprotective and anti-inflammatory effects of the adenosine A(2A) receptor antagonist ST1535 in a MPTP mouse model of Parkinson's disease. Synapse. 2011 Mar;65(3):181-8. 4. Francesca Bartoccini, et al. Direct B-alkyl Suzuki-Miyaura cross-coupling of 2-halopurines. Practical synthesis of ST1535, a potent adenosine A2A receptor antagonist. J Org Chem. 2010 Aug 6;75(15):5398-401.

Related compound libraries

This product is contained In the following compound libraries：

GPCR Compound Library Anti-Neurodegenerative Disease Compound Library Inhibitor Library Bioactive Compound Library ReFRAME Related Library Neurotransmitter Receptor Compound Library Neuronal Signaling Compound Library Bioactive Compounds Library Max

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Keywords

ST-1535 496955-42-1 GPCR/G Protein Neuroscience Adenosine Receptor ST1535 ST 1535 inhibitor inhibit

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