Desmethyl Carvedilol

Desmethyl Carvedilol

CAT N°: 35411
Price:

From 100.00 85.00

Desmethyl carvedilol is an active metabolite of the non-selective ?-adrenergic receptor (?-AR) antagonist carvedilol (Item No. 15418).{49063,61991,61992} It is formed from carvedilol by the cytochrome P450 (CYP) isoform CYP2C9.{49063} Desmethyl carvedilol inhibits store-overload-induced calcium release in HEK293 cells expressing the ryanodine receptor 2 (RyR2) R4496C (RyR2R4496C) mutation (IC50 = 7.62 µM), a mutation that results in spontaneous calcium release from the endoplasmic reticulum.{61991} It reduces increases in heart rate and prevents decreases in diastolic blood pressure induced by isoproterenol (Item No. 15592) in conscious rabbits (ED50s = 32 and 5 µg/kg, respectively).{61992}

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • 2-[2-[[3-(9H-carbazol-4-yloxy)-2-hydroxypropyl]amino]ethoxy]-phenol
  • Correlated keywords
    • ODMC BM14242 ?AR P-450 CYP-2C9 HEK293
  • Product Overview:
    Desmethyl carvedilol is an active metabolite of the non-selective ?-adrenergic receptor (?-AR) antagonist carvedilol (Item No. 15418).{49063,61991,61992} It is formed from carvedilol by the cytochrome P450 (CYP) isoform CYP2C9.{49063} Desmethyl carvedilol inhibits store-overload-induced calcium release in HEK293 cells expressing the ryanodine receptor 2 (RyR2) R4496C (RyR2R4496C) mutation (IC50 = 7.62 µM), a mutation that results in spontaneous calcium release from the endoplasmic reticulum.{61991} It reduces increases in heart rate and prevents decreases in diastolic blood pressure induced by isoproterenol (Item No. 15592) in conscious rabbits (ED50s = 32 and 5 µg/kg, respectively).{61992}

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