A selective estrogen receptor modulator

Lasofoxifene – 10 mg

Brand:
Cayman
CAS:
180916-16-9
Storage:
-20
UN-No:
Non-Hazardous - /

Lasofoxifene is a third-generation, non-steroidal selective estrogen receptor modulator (SERM). It selectively binds to human ERα 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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Description

A selective estrogen receptor modulator, selectively binds to human ERα (IC50 = 1.5 nM); inhibits bone loss in ovariectomized rats; in clinical studies 0.5 mg/day associated with reduced risks of nonvertebral and vertebral fractures, ER-positive breast cancer, coronary heart disease, and stroke and increased risk of venous thromboembolic events; an inverse agonist at the CB2 cannabinoid receptor,

Formal name: (5R,6S)-5,6,7,8-tetrahydro-6-phenyl-5-[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]-2-naphthalenol

Synonyms:  CP 336,156

Molecular weight: 413.6

CAS: 180916-16-9

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Inverse Agonists||Research Area|Endocrinology & Metabolism|Hormones & Receptors|Estrogens & Progestins||Research Area|Neuroscience|Cannabinoid Research|CB1 & CB2 Receptors

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