|
Appearance
|
Pale yellow powder
|
|
Residue on ignition
|
0.07%
|
|
Loss on drying
|
0.35% |
| Assay |
98.54% |
RL (LY156758, Keoxifene) HCl is an orally active and selective estrogen receptor modulator (SERM) that inhibits phtharazine oxidation activity catalyzed by cytoplasmic aldehyde oxidase in humans with an IC50 of 5.7 nM
RL has been shown to be a potent, non-competitive inhibitor of phthalezine, vanillin, and nicotine-δ'(5')-imide ion oxidation with Ki values of 0.87 nM and 1.2 nMand to 1.4 nM, respectively. RL is also a non-competitive inhibitor that inhibits the reduction of hydroxamic acid-containing compounds catalyzed by aldehyde dehydrogenated chemicalbook enzymes with a Ki value of 51 nM. RL activates the TGFβ3 promoter as a complete agonist at nanomolar concentrations, and in transient transfection experiments, RL acts as a pure estrogen antagonist to inhibit the expression of estrogen-responsive elements containing a yolk production hormone promoter.
In rat femurs, RL reconstructs bone mineral density and TGFbeta3 mRNA expression. RL (0.1 mg/kg-10 mg/kg, p.o. for 5 weeks) increases femoral and tibial mineral density in oophorectomy rats. In oophorectomy rats, RL decreases the cholesterol content in serum Chemicalbook with an ED50 of 0.2 mg/kg. RL causes a significant lack of estrogen effect in uterine tissues. In oophorectomy rats, RL blocks alterations in osteopenia and bone growth, bone remodeling, and blood cholesterol content, but is less effective at reducing bone formation and does not prevent uterine atrophy.
Product Description
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