Formulation: A solid
Formal Name: trans-4-[(2-phenyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]-cyclohexanol
Purity: ≥98%
Formula Markup: C18H20N4O
Formula Weight: 308,4
Shelf life (days): 1460
CAS Number: 251945-92-3
Notes: 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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