A third-generation SERM that selectively binds to human ERα (IC50 = 1.5 nM) and inhibits bone loss in ovariectomized rats; used in the treatment of postmenopausal osteoporosis and ER-positive breast cancer; also acts as an inverse agonist at the CB2 cannabinoid receptor

Lasofoxifene (tartrate) – 5 mg

Brand:
Cayman
CAS:
190791-29-8
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 third-generation SERM that selectively binds to human ERα (IC50 = 1.5 nM) and inhibits bone loss in ovariectomized rats; used in the treatment of postmenopausal osteoporosis and ER-positive breast cancer; also acts as 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, (2S,3S)-2,3-dihydroxybutanedioate

Synonyms:  CP 336,156

Molecular weight: 563.6

CAS: 190791-29-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology||Research Area|Endocrinology & Metabolism|Bone Growth & Remodeling||Research Area|Endocrinology & Metabolism|Hormones & Receptors|Estrogens & Progestins||Research Area|Neuroscience|Cannabinoid Research|CB1 & CB2 Receptors

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