| Stereochemistry | ABSOLUTE |
| Molecular Formula | C18H20O5S |
| Molecular Weight | 348.413 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 3 / 3 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
C[C@]12CC[C@H]3C(=CCC4=C3C=CC(OS(O)(=O)=O)=C4)[C@@H]1CCC2=O
InChI
InChIKey=YJBYRYVLFAUXBJ-HFTRVMKXSA-N
InChI=1S/C18H20O5S/c1-18-9-8-14-13-5-3-12(23-24(20,21)22)10-11(13)2-4-15(14)16(18)6-7-17(18)19/h3-5,10,14,16H,2,6-9H2,1H3,(H,20,21,22)/t14-,16+,18+/m1/s1
Equilin sulfate is one of the main component, which is responsible for the pharmacological action of the PREMARIN, conjugated estrogens tablets. Premarin is used to treat the moderate to severe vasomotor symptoms, vulvar and vaginal atrophy due to menopause. It is also used to treat hypoestrogenism due to hypogonadism, castration or primary ovarian failure; to treat breast cancer and advanced androgen-dependent carcinoma of the prostate (for Palliation Only). In addition, premarin is used to prevent postmenopausal osteoporosis. Equilin sulfate is a prodrug, which is hydrolyzed to the corresponding free estrogen equilin, an inhibitor of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1). Human 17beta-HSD1 catalyzes the reduction of inactive estrone (E1) to the active 17beta-estradiol in breast tissues, is a key enzyme responsible for elevated levels of E2 in breast tumor tissues. Thus equilin reduce the E2 levels in breast tissues and hence the reduce risk of estrogen-dependent breast cancer.
Approval Year
Doses
PubMed
Patents
Sample Use Guides
In order to determine the relative potency of equilin sulfate (EqS) 15 women received oral doses of EqS (0.15, 0.31, and 0.625 mg) for 25 days. Doses of 0.31 and 0.625 mg significantly stimulated hepatic globulins. This stimulatory effect ranged from being 1.5 to 8 times greater than the effects of comparable doses of estrone sulfate and conjugated equine estrogens.
Route of Administration:
Oral
SALT/SOLVATE (PARENT)
SUBSTANCE RECORD
