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KI0771Raloxifene HCl50 mg$154
Raloxifene HCl100 mg$272

Chemical Characteristic

Product NameRaloxifene HCl
SynonymsEvista
CAS No.82640-04-8
Molecular Weight 510.04
FormulaC28H28ClNO4S
Chemical Structure
DocumentsHNMR COA LCMS

Biological activities

Raloxifene HCl is a hydrochloride salt form of raloxifene which is an oral selective estrogen receptor modulator. Raloxifene inhibits the induction of progesterone receptor (PR) by estradiol with an IC50 of 1 nM.[1] Raloxifene concentration-dependently inhibits transient outward currents (Ito 1) with an IC50 of 0.9 µM. Raloxifene at the dose of 1 µM decreases Ito1 by 40.2%. Raloxifene remarkably suppresses ultra-rapid delayed rectifier potassium currents (IKur) with an IC50 of 0.7 µM. Raloxifene at 1 µM decreases IKur by 57.3%.[2] Raloxifene blocks IhERG (cloned hERG channel) with an IC50 of 1.1 µM. Raloxifene decreases recombinant human cardiac KCNQ1/KCNE1 channel (IKs) with an IC50 of 4.8 µM.[3] Raloxifene prevents the proliferation of the human breast cancer cell line, MCF-7, with an IC50 of 0.2 nM. Raloxifene suppresses loss of bone with EC50 of 0.3 mg/kg/day for both the axial and appendicular skeleton.[4] Raloxifene induces coronary arterial relaxation in male and female coronary arteries by an endothelium-dependent and estrogen receptor閳ユ徆ependent mechanism involving nitric oxide in rabbits.[5] Raloxifene prevents the mRNA expression of interleukin (IL)-1β and IL-6 at a low concentration.[6] After intra-jejunal (i.j.) administration, raloxifene is extensively metabolized in the gut.[7]

Protocols

In vivo: Raloxifene is dissolved in DMSO to a final concentration of 20 mg/mL.[7]

References

[1] Fitzpatrick SL, et al. Effect of estrogen agonists and antagonists on induction of progesterone receptor in a rat hypothalamic cell line. Endocrinology. 1999, 140(9): 3928-3937. 閵嗏偓閵嗏偓
[2] Liu H, et al. Raloxifene inhibits transient outward and ultra-rapid delayed rectifier potassium currents in human atrial myocytes. Eur J Pharmacol. 2007, 563(1-3): 61-68. 閵嗏偓閵嗏偓
[3] Liu H, et al. The selective estrogen receptor modulator raloxifene inhibits cardiac delayed rectifier potassium currents and voltage-gated sodium current without QTc interval prolongation. Pharmacol Res. 2010, 62(5): 384-90. 閵嗏偓閵嗏偓
[4] Sato M, et al. Raloxifene: A selective estrogen receptor modulator. Journal of Bone and Mineral Metabolism. 1994, 12(2), S9-S20. 閵嗏偓閵嗏偓
[5] Figtree GA, et al. Raloxifene acutely relaxes rabbit coronary arteries in vitro by an estrogen receptor-dependent and nitric oxide-dependent mechanism. Circulation. 1999, 100(10): 1095-1101. 閵嗏偓閵嗏偓
[6] Taranta A, et al. The selective estrogen receptor modulator raloxifene regulates osteoclast and osteoblast activity in vitro. Bone. 2002, 30(2): 368-376. 閵嗏偓閵嗏偓
[7] Thörn HA, et al. Extensive intestinal glucuronidation of raloxifene in vivo in pigs and impact for oral drug delivery. Xenobiotica. 2012, 42(9): 917-928. 閵嗏偓閵嗏偓

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