Lasofoxifene

Lasofoxifene

CAT N°: 21754
Price:

From 182.00 154.70

Lasofoxifene is a third-generation, non-steroidal selective estrogen receptor modulator (SERM). It selectively binds to human ER? with an IC50 value of 1.5 nM and inhibits bone loss in ovariectomized rats.{28785} In clinical studies of postmenopausal osteoporosis, 0.5 mg/day lasofoxifene was associated with reduced risks of nonvertebral and vertebral fractures, ER-positive breast cancer, coronary heart disease, and stroke but an increased risk of venous thromboembolic events.{28786,28787} Lasofoxifene has also been shown to act as an inverse agonist at the CB2 cannabinoid receptor, indicating its potential to be repurposed as a therapeutic for indications wherein CB2 is a target.{28788}

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • (5R,6S)-5,6,7,8-tetrahydro-6-phenyl-5-[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]-2-naphthalenol
  • Correlated keywords
    • CP336156 CP336,156 336156 ERa ? ER a CB 2
  • Product Overview:
    Lasofoxifene is a third-generation, non-steroidal selective estrogen receptor modulator (SERM). It selectively binds to human ER? with an IC50 value of 1.5 nM and inhibits bone loss in ovariectomized rats.{28785} In clinical studies of postmenopausal osteoporosis, 0.5 mg/day lasofoxifene was associated with reduced risks of nonvertebral and vertebral fractures, ER-positive breast cancer, coronary heart disease, and stroke but an increased risk of venous thromboembolic events.{28786,28787} Lasofoxifene has also been shown to act as an inverse agonist at the CB2 cannabinoid receptor, indicating its potential to be repurposed as a therapeutic for indications wherein CB2 is a target.{28788}

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