An adenosine A1 receptor antagonist (Ki = 1 nM); selective for adenosine A1 over A2A

Derenofylline – 5 mg

Brand:
Cayman
CAS:
251945-92-3
Storage:
-20
UN-No:
Non-Hazardous - /

Derenofylline is an adenosine A1 receptor antagonist (Ki = 1 nM).{53110} It is selective for adenosine A1 over A2A, A2B, and A3 receptors (Kis = 398, 3,981, and 200 nM, respectively). It decreases adenosine A1 receptor-mediated adenosine-induced bradycardia in rats (ED50 = 0.49 mg/kg) but reduces A2 receptor-mediated adenosine-induced hypotension by only 44.6% when administered at an intravenous dose of 5 mg/kg. It prevents increases in heart levels of collagen I and III in nephrectomized rats when administered at a dose of 10 mg/kg per day. Derenofylline also reduces relative plaque counts in a Zika virus plaque-forming assay in A549 cells (IC50 = 58.6 nM) in an adenosine A1 receptor-independent manner without inducing cytotoxicity when used at concentrations less than 10 µM.{42519}  

 

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Description

An adenosine A1 receptor antagonist (Ki = 1 nM); selective for adenosine A1 over A2A, A2B, and A3 receptors (Kis = 398, 3,981, and 200 nM, respectively); decreases adenosine A1 receptor-mediated adenosine-induced bradycardia in rats (ED50 = 0.49 mg/kg) but reduces A2 receptor-mediated adenosine-induced hypotension by only 44.6% at an intravenous dose of 5 mg/kg; prevents increases in heart levels of collagen I and III in nephrectomized rats at 10 mg/kg per day; reduces relative plaque counts in a Zika virus plaque-forming assay in A549 cells (IC50 = 58.6 nM) in an adenosine A1 receptor-independent manner

Formal name: trans-4-[(2-phenyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]-cyclohexanol

Synonyms:  SLV 320

Molecular weight: 308.4

CAS: 251945-92-3

Purity: ≥98%

Formulation: A solid

Product Type|Biochemicals|Antivirals||Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cardiovascular System|Cardiovascular Diseases|Hypotension||Research Area|Cardiovascular System|Heart|Arrhythmia||Research Area|Cardiovascular System|Kidney & Renal Disease||Research Area|Immunology & Inflammation||Research Area|Infectious Disease|Viral Diseases|Zika

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