A selective estrogen receptor modulator
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Raloxifene (hydrochloride)

Item No. 10011620

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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
Synonyms
  • Keoxifene
  • LY156758
Molecular Formula
C28H27NO4S • HCl
Formula Weight
510.0
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 15 mg/mlDMSO:PBS (pH 7.2) (1:2): 0.3 mg/mlEthanol: 0.1 mg/ml
λmax
222, 287 nm
SMILES
OC1=CC=C(C(C(C2=CC=C(OCCN3CCCCC3)C=C2)=O)=C(C4=CC=C(O)C=C4)S5)C5=C1.Cl
InChi Code
InChI=1S/C28H27NO4S.ClH/c30-21-8-4-20(5-9-21)28-26(24-13-10-22(31)18-25(24)34-28)27(32)19-6-11-23(12-7-19)33-17-16-29-14-2-1-3-15-29;/h4-13,18,30-31H,1-3,14-17H2;1H
InChi Key
BKXVVCILCIUCLG-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    50 mg

    $36

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    100 mg

    $68

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    250 mg

    $153

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    500 mg

    $268

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    Product Description

    Raloxifene is a selective estrogen receptor modulator (SERM) that binds to the estrogen receptor with an IC50 value of 0.4 nM.1 It exhibits estrogenic activity in bone cells without stimulating breast or uterine tissues.2 Raloxifene 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).2,3 Raloxifene also inhibits the voltage-gated potassium channel Kv4.3 in an estrogen-independent manner (IC50 = 2 µM).4 Formulations containing raloxifene have been shown to reduce bone resorption and promote bone formation in post-menopausal women.5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Sun, D., Jones, N.R., Manni, A., et al. Characterization of raloxifene glucuronidation: Potential role of UGT1A8 genotype on raloxifene metabolism in vivo. Cancer Prev. Res. (Phila.) 6(7), 719-730 (2013).

    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(1), 63-69 (1994).

    3. Wong, C.M., Yung, L.M., Leung, F.P., et al. Raloxifene protects endothelial cell function against oxidative stress. Br. J. Pharmac. 155(3), 326-334 (2008).

    4. Chae, Y.J., Kim, D.H., Lee, H.J., et al. Raloxifene inhibits cloned Kv4.3 channels in an estrogen receptor-independent manner. Pflugers Arch. 467(8), 1663-1676 (2015).

    5. Özmen, B., Kirmaz, C., Aydin, K., et al. Influence of the selective oestrogen receptor modulator (raloxifene hydrochloride) on IL-6, TNF-α, TGF-ß1 and bone turnover markers in the treatment of postmenopausal osteoporosis. Eur. Cyto. Netw. 18(3), 148-153 (2007).