A non-selective adenosine receptor antagonist (Kbs = 83

Xanthine amine congener – 10 mg

Brand:
Cayman
CAS:
96865-92-8
Storage:
-20
UN-No:
Non-Hazardous - /

Xanthine amine congener (XAC) is a non-selective adenosine receptor antagonist with Kb values of 83, 25, and 15 nM for rat PC12 cells, human platelets that endogenously express adenosine A2A receptors, and rat fat cells that endogenously express A1 receptors, respectively.{41674} It reduces adenylate cyclase activity stimulated by 5′-N-ethylcarboxamidoadenosine (NECA; Item No. 21420) in human platelets (EC50s = 1 and 0.31 μM in the presence and absence of XAC, respectively). XAC also reverses R-PIA-induced inhibition of isoproterenol-stimulated adenylate cyclase activity in rat fat cell membranes (IC50s = 146 and 26 nM in the presence and absence of XAC, respectively). In vivo, XAC reverses reductions in heart rate and blood pressure induced by 2-chloro-3-deazaadenosine (2-CADO; Item No. 9000787), R-PIA, and NECA in rats when administered at doses ranging from 0.1 to 1.0 mg/kg.{41675} XAC (39.8 mg/kg) also induces convulsions in mice.{41676}  

 

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SKU: 23077 - 10 mg Category:

Description

A non-selective adenosine receptor antagonist (Kbs = 83, 25, and 15 nM for rat PC 12 cells, human platelets, and rat fat cells, respectively); reduces NECA-stimulated adenylate cyclase activity in human platelets (EC50s = 1 and 0.31 μM in the presence and absence of XAC, respectively); reverses R-PIA-induced inhibition of isoproterenol-stimulated adenylate cyclase activity in rat fat cell membranes (IC50s = 146 and 26 nM in the presence and absence of XAC, respectively); reverses 2-CADO-, R-PIA-, and NECA-induced reductions in heart rate and blood pressure in rats (0.1-1.0 mg/kg); induces convulsions in mice (39.8 mg/kg)

Formal name: N-(2-aminoethyl)-2-[4-(2,3,6,7-tetrahydro-2,6-dioxo-1,3-dipropyl-1H-purin-8-yl)phenoxy]-acetamide

Synonyms:  XAC

Molecular weight: 428.5

CAS: 96865-92-8

Purity: ≥98%

Formulation: A solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cardiovascular System|Cardiovascular Diseases|Hypotension||Research Area|Cardiovascular System|Heart|Arrhythmia||Research Area|Neuroscience|Seizure Disorders

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