A potent antagonist for the human IP (prostacyclin) receptor that antagonizes the carbaprostacyclin-induced activation of human neuroblastoma adenylate cyclase

CAY10441 – 10 mg

Brand:
Cayman
CAS:
221529-58-4
Storage:
-20
UN-No:
Non-Hazardous - /

Recently, a series of relatively simple compounds were found to be high-affinity ligands and functional antagonists for the human IP (prostacyclin) receptor.{11836} CAY10441 is one of the more potent of these. CAY10441 antagonizes the carbaprostacyclin-induced activation of human neuroblastoma adenylate cyclase, blocking cyclic AMP accumulation in a dose-dependent manner. Likewise, it inhibits the binding of tritiated iloprost to rodent neuroblastoma cells with a Ki of about 1.5 nM. At levels between 2-20 mg/kg in rats, CAY10441 shows significant analgesic activity in standard antinociceptive assays.{11836}  

 

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SKU: 10005186 - 10 mg Category:

Description

A potent antagonist for the human IP (prostacyclin) receptor that antagonizes the carbaprostacyclin-induced activation of human neuroblastoma adenylate cyclase, blocking cAMP accumulation in a dose-dependent manner; inhibits the binding of tritiated iloprost to rodent neuroblastoma cells (Ki = about 1.5 nM); shows significant analgesic activity in standard antinociceptive assays at levels between 2-20 mg/kg

Formal name: 4,5-dihydro-N-[4-[[4-(1-methylethoxy)phenyl]methyl]phenyl]-1H-imadazol-2-amine

Synonyms:  RO1138452

Molecular weight: 309.4

CAS: 221529-58-4

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Lipid Biochemistry|Cyclooxygenase Pathway||Research Area|Neuroscience|Pain Research

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