LASOFOXIFENE HCL Struktur

LASOFOXIFENE HCL

Bezeichnung:LASOFOXIFENE HCL

CAS-Nr190791-29-8

Englisch Name:LASOFOXIFENE HCL

CBNumberCB91516053

SummenformelC32H37NO8

Molgewicht563.65

MOL-Datei190791-29-8.mol

LASOFOXIFENE HCL physikalisch-chemischer Eigenschaften

Schmelzpunkt	185 °C(dec.)
storage temp.	2-8°C
Löslichkeit	DMSO: soluble10mg/mL, clear
Aggregatzustand	powder
Farbe	white to beige

Sicherheit

WGK Germany	3
HS Code	2933.99.7500

Gefahreninformationscode (GHS)

LASOFOXIFENE HCL Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden
disintegrant, enteric coating, sustained release formulations
Biologische Aktivität
lasofoxifene (tartrate) is a third-generation, nonsteroidal selective estrogen receptor modulator (serm).estrogen receptors are activated by the hormone estrogen (17β-estradiol). serms are characterized by having estrogen agonist action in some tissues while acting as estrogen antagonists in others [1][2].lasofoxifene, also known as cp 336,156, is a third-generation, nonsteroidal selective estrogen receptor modulator. lasofoxifene bound with high affinity to the human estrogen receptor-α with ic50 value of 1.5 nm [1]. lasofoxifene is also a cb2 inverse agonist [4].in aged female rats, lasofoxifene decreased total serum cholesterol and fat body mass, and no uterine hypertrophy was observed. in 5-month-old ovariectomized (ovx) sprague-dawley female rats, lasofoxifene completely prevented ovx-induced increases in body weight gain, total serum cholesterol, and serum osteocalcin. cp-336,156 completely prevented ovx-induced bone loss and inhibited the increased bone turnover associated with estrogen deficiency in lumbar vertebrae, proximal tibiae, and distal femora [1].in postmenopausal women with osteoporosis, lasofoxifene reduced risks of nonvertebral and vertebral fractures, er-positive breast cancer, coronary heart disease, and stroke but an increased risk of venous thromboembolic events [2][3].
Biochem/physiol Actions
Lasofoxifene is a third-generation selective estrogen receptor modulator (SERM).
Einzelnachweise
[1]. ke hz, paralkar vm, grasser wa, et al. effects of cp-336,156, a new, nonsteroidal estrogen agonist/antagonist, on bone, serum cholesterol, uterus and body composition in rat models. endocrinology. 1998 apr;139(4):2068-76.
[2]. cummings sr, ensrud k, delmas pd, et al. lasofoxifene in postmenopausal women with osteoporosis. n engl j med. 2010 feb 25;362(8):686-96.
[3]. gennari l, merlotti d, nuti r. selective estrogen receptor modulator (serm) for the treatment of osteoporosis in postmenopausal women: focus on lasofoxifene. clin interv aging. 2010 feb 2;5:19-29.
[4]. kumar p, song zh. cb2 cannabinoid receptor is a novel target for third-generation selective estrogen receptor modulators bazedoxifene and lasofoxifene. biochem biophys res commun. 2014 jan 3;443(1):144-9.

LASOFOXIFENE HCL Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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