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Raloxifene (hydrochloride)

Cayman Chemical Item Number 10011620

Evista; LY156758; Keoxifene (hydrochloride) (CAS 82640-04-8)

Raloxifene (hydrochloride) (CAS 82640-04-8)

See more	Receptor Antagonist (45) Bone-Related Research (30) Cancer (606)

Description

Selective estrogen receptor modulators (SERMs) are a class of pharmacologically active ER ligands that exert agonist and antagonist effects on various estrogen target tissues.¹ They are designed to promote the beneficial actions of estrogen (e.g., bone maintenance and remodeling) while preventing its detrimental effects (e.g., growth of breast and endometrial cancers). Raloxifene, marketed under the name Evista, is a SERM that exhibits estrogenic activity in bone cells without stimulating breast or uterine tissues.² It has been approved for clinical use for prevention and treatment of postmenopausal osteoporosis. When administered at 60 mg/day for 12 weeks to postmenopausal, osteoporotic women, raloxifene reduced bone resportion, and promoted bone formation by decreasing serum levels of interleukin-6 and parathyroid hormone and increasing serum levels of 25-hydroxy vitamin D.³ Raloxifene reportedly guards endothelial cells obtained from rat aortic rings against oxidative insult (1 µM) and lowers serum cholesterol in ovariectomized rodents (ED₅₀ = 0.2 mg/kg).^4,2

1 Skouby, S.O. Criteria for the selection of an optimal estrogen replacement.. Gynecol Endocrinol 15 60-67 (2001).

2 Black, L.J., Sato, M., Rowley, E.R., et al. Raloxifene (LY139481 HCI) prevents bone loss and reduces serum cholesterol without causing uterine hypertrophy in ovariectomized rats. J Clin Invest 93 63-69 (1994).

3 Özmen, B., Kirmaz, C., Aydin, K., et al. Influence of the selective oestrogen receptor modulator (raloxifene hydrochloride) on IL-6, TNF-a, TGF-b1 and bone turnover markers in the treatment of postmenopausal osteoporosis. Eur Cytokine Netw 18 148-153 (2007).

4 Wong, C.M., Yung, L.M., Leung, F.P., et al. Raloxifene protects endothelial cell function against oxidative stress. Br J Pharmacol 155 326-334 (2008).

Synonyms	Evista LY156758 Keoxifene (hydrochloride)
Formal Name	[6-hydroxy-2-(4-hydroxyphenyl)benzo[b]thien-3-yl][4-[2-(1-piperidinyl)ethoxy]phenyl]-methanone, monohydrochloride
CAS Number	82640-04-8
Molecular Formula	C₂₈H₂₇NO₄S · HCl
Formula Weight	510.2
Formulation	A crystalline solid
Purity	≥98%
Stability	2 years
Storage	-20°C
Shipping	Room temperature in continental US; may vary elsewhere
SMILES	Copy SMILES to clipboard Oc1ccc(cc1)c1sc2cc(O)ccc2c1C(=O)c1ccc(OCCN2CCCCC2)cc1 Cl

Background Reading

Wong, C.M., Yung, L.M., Leung, F.P., et al. Raloxifene protects endothelial cell function against oxidative stress. Br J Pharmacol 155 326-334 (2008).

Özmen, B., Kirmaz, C., Aydin, K., et al. Influence of the selective oestrogen receptor modulator (raloxifene hydrochloride) on IL-6, TNF-a, TGF-b1 and bone turnover markers in the treatment of postmenopausal osteoporosis. Eur Cytokine Netw 18 148-153 (2007).

Black, L.J., Sato, M., Rowley, E.R., et al. Raloxifene (LY139481 HCI) prevents bone loss and reduces serum cholesterol without causing uterine hypertrophy in ovariectomized rats. J Clin Invest 93 63-69 (1994).

Skouby, S.O. Criteria for the selection of an optimal estrogen replacement.. Gynecol Endocrinol 15 60-67 (2001).

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Size	Price	Quantity	Subtotal
50 mg	$32.00		$0.00
100 mg	$61.00		$0.00
250 mg	$144.00		$0.00
500 mg	$256.00		$0.00
Bulk	Contact
		Cart Total	$0.00

Pricing updated 2012-02-12. Prices are subject to change without notice.

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