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Equilin (7-Dehydroestrone) Sale

(Synonyms: 马烯雌酮; 7-Dehydroestrone) 目录号 : GC34006

Equilin (7-Dehydroestrone) (7-Dehydroestrone) 是一大类雌激素物质的重要成员,在化学上与二甲双胍 (oestrone) 相关。

Equilin (7-Dehydroestrone) Chemical Structure

Cas No.:474-86-2

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产品描述

Equilin is one of the estrogens present in the mixture of estrogens isolated from horse urine.

Chemical Properties

Cas No. 474-86-2 SDF
别名 马烯雌酮; 7-Dehydroestrone
Canonical SMILES C[C@]1([C@](CC2)([H])C3=CCC4=C(C=CC(O)=C4)[C@@]3([H])CC1)C2=O
分子式 C18H20O2 分子量 268.35
溶解度 DMSO: 100 mg/mL (372.65 mM) 储存条件 Store at -20°C
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Research Update

Metabolism of Equilin sulfate in the dog

J Steroid Biochem Mol Biol 1995 Nov;55(2):271-8.PMID:7495708DOI:10.1016/0960-0760(95)00161-r.

The metabolism of Equilin sulfate was determined in female dogs receiving 2.5 mg/kg of [3H]Equilin sulfate alone or in a preparation that contained all the components that are present in the conjugated equine estrogen product Premarin. The pharmacokinetic parameters of total radioactivity indicated that the drug is rapidly absorbed and it has a moderate half-life in plasma. The total radioactivity in plasma following administration of [3H]Equilin sulfate as part of a mixture of conjugated equine estrogens had significantly lower peak concentration (Cmax), a lower area under the curve (AUC), a longer terminal half-life (t1/2) and a longer mean residence time (MRT) than when [3H]Equilin sulfate was given alone, indicating that the other components in the conjugated equine estrogen preparation altered the pharmacokinetics of Equilin sulfate. An average of 26.7 +/- 4.4% of the administered radioactive dose was excreted in urine of dogs receiving [3H]Equilin sulfate. Again, a significantly lower percentage (21.4 +/- 6.3%, P = 0.023) was eliminated in urine of dogs receiving [3H]Equilin sulfate in the conjugated equine estrogen preparation, indicating that the absorption of Equilin sulfate was perhaps altered by the other components in the conjugated equine estrogen preparation. Metabolite profiles of plasma and urine were similar. Equilin, equilenin, 17 beta-dihydroequilenin, 17 beta-dihydroequilin, 17 alpha-dihydroequilenin and 17 alpha-dihydroequilin were present in both matrices. 17 beta-Dihydroequilin and Equilin were the two major chromatographic peaks in plasma samples. 17 beta-Dihydroequilenin and 17 beta-dihydroequilin were the major metabolites in urine. In conclusion, following oral administration of [3H]Equilin sulfate to dogs, the radioactivity is rapidly absorbed. The disposition of Equilin sulfate is altered by the other components that are present in the conjugated equine estrogen preparation Premarin. The reduction of the 17-keto group and aromatization of ring-B are the major metabolic pathways of Equilin in the dog.

Pharmacokinetics of Equilin and Equilin sulfate in normal postmenopausal women and men

J Clin Endocrinol Metab 1983 May;56(5):1048-56.PMID:6300173DOI:10.1210/jcem-56-5-1048.

The MCRs of Equilin sulfate and Equilin were determined in normal postmenopausal women and a normal man by single iv injections of either [3H]Equilin sulfate or [3H] Equilin. After the administration of [3H]Equilin sulfate, blood was drawn at various time intervals, and the plasma obtained was fractionated into the unconjugated, sulfate, and glucuronide fractions. The bulk of radioactivity was present in the sulfate fraction, and from this, [3H]Equilin sulfate, [3H]17 beta-dihydro-equilin sulfate, [3H]equilenin sulfate, and [3H]17 beta-dihydroequilenin sulfate were isolated and purified, and their concentrations were measured. The disappearance of radioactivity from plasma as Equilin sulfate can be described as a function that is the sum of two exponentials. The initial fast component (half-life, 5.2 +/- 1.2 min) represents distribution and transfer from a space, with a mean volume of 12.4 +/- 1.6 liters. The mean value for the rate constant of total removal from the initial volume is 163 +/- 19 U/day, of which 15.8 +/- 2% is irreversible. The mean half-life of the slower component of Equilin sulfate is 190 +/- 23 min, and the mean MCR is 176 +/- 44 liters/day . m2. Similarly, after the administration of [3H]Equilin to a normal postmenopausal woman and a man, the disappearance of radio-activity from plasma as Equilin could be fitted by a single straight line, consistent with a one-compartment system. The half-life of Equilin was approximately 19-27 min, and the MCR of Equilin was calculated to be 1982 liters/day/m2 in the normal man and 3300 liters/day/m2 in the normal postmenopausal woman. The bulk of [3H]Equilin was very rapidly metabolized to mainly Equilin sulfate. Small amounts of 17 beta-dihydroequilin sulfate and 17 beta-dihydroequilin were also isolated from the plasma. The in vivo formation of 17 beta-dihydroequilin and its sulfate may be of importance, as this estrogen is approximately 8 times more potent as a uterotropic agent than Equilin sulfate.

Separation and detection of the isomeric equine conjugated estrogens, Equilin sulfate and delta8,9-dehydroestrone sulfate, by liquid chromatography--electrospray-mass spectrometry using carbon-coated zirconia and porous graphitic carbon stationary phases

J Chromatogr A 2005 Aug 12;1083(1-2):42-51.PMID:16078686DOI:10.1016/j.chroma.2005.05.092.

Equilin-3-sulfate and delta8,9-dehydroestrone-3-sulfate are two isomers found in equine conjugated estrogens that differ in structure only by the position of a double bond in the steroid B-ring. These geometric isomers were not resolved on a C18 column during the analysis of conjugated estrogen drug products by LC-MS using acetonitrile-ammonium acetate buffer as the mobile phase. While no separations of these two isomers were observed on C18 or other alkyl-bonded silica based phases using a variety of mobile phase conditions, partial separations were achieved on phenyl bonded silica phases with a resolution of 1.5 on a diphenyl phase, and baseline separations were readily achieved on two carbonaceous phases with resolutions routinely exceeding three on graphitic carbon-coated zirconia (Zr-CARB) and resolutions as high as 19 on porous graphitic carbon (Hypercarb). An examination of a selected few conjugated estrogens in the complex drug substance by LC-MS on Hypercarb is presented.

Metabolism of [3H]equilin-[35S]sulfate and [3H]Equilin sulfate after oral and intravenous administration in normal postmenopausal women and men

J Clin Endocrinol Metab 1989 Apr;68(4):757-65.PMID:2921309DOI:10.1210/jcem-68-4-757.

The absorption of Equilin sulfate and Equilin from the gastrointestinal tract was determined in normal men after the ingestion of [3H]equilin-[35S]sulfate or a mixture of [3H]Equilin and equilin-[35S]sulfate, while the metabolism of Equilin sulfate was investigated after iv administration of [3H]Equilin sulfate to postmenopausal women. After the oral administration of [3H]equilin-[35S]sulfate, Equilin sulfate containing both 3H and 35S was isolated from plasma; however, only in the first sample taken at 10 min was the 3H/35S ratio the same as that of the [3H]equilin-[35S]sulfate ingested. The 3H/35S ratio then increased, and by 12 h only traces of equilin-[35S]sulfate were detectable. Similarly, after the ingestion of [3H]Equilin and equilin-[35S]sulfate, [3H]equilin-[35S]sulfate was isolated from plasma. The 3H/35S ratio was at all time points greater than the 3H/35S ratio of the ingested mixture. Analysis of urine indicated that over 98% of 35S was not associated with any steroid and was most likely inorganic sulfate. After iv administration of [3H] Equilin sulfate to postmenopausal women, Equilin, equilenin, 17 beta-dihydroequilin, and 17 beta-dihydroequilenin were isolated from the urine. These results indicate that 1) some of the orally administered Equilin sulfate was absorbed from the gut without prior hydrolysis, 2) some Equilin sulfate was hydrolyzed in the gut before absorption; 3) Equilin was absorbed more efficiently than Equilin sulfate; 4) Equilin absorbed was readily sulfated and circulated in this form; and 5) Equilin sulfate was extensively metabolized, and the metabolites were excreted in the urine mainly conjugated with glucuronic acid.

The metabolism of Equilin in normal men

J Steroid Biochem 1982 Aug;17(2):217-23.PMID:7109607DOI:10.1016/0022-4731(82)90125-x.

Healthy adult males received either [3H]-equilin intravenously (one subject) or a larger mass of unlabelled Equilin orally (three subjects). Blood samples were taken at 20, 40, 60, 90 and 120 min and every h thereafter until eight h after injection. Urine was collected in 24 h aliquots for five days from all subjects. The half-life of the disappearance of the unconjugated radioactivity from blood was 30 min and that in the conjugated sulfate fraction was 5 1/2 h. Approximately 50% of the injected radioactivity was recovered in the urine over 5 days. After extraction, hydrolysis and fractionation, most (83%) of the radioactive material found in the urine was present in the glucuronide fraction while only 2 and 6% were present in the unconjugated and sulfate fractions, respectively. The three fractions were combined for further isolation and identification of the metabolites. Radiochemically pure Equilin, equilenin, 17 beta-dihydro-equilin and 17 beta-dihydroequilenin were isolated and identified but the largest fraction of radioactivity (70.5%) was present in the form of metabolites which are more polar than any of the known ring B unsaturated estrogens. These appear to be polyhydroxy 17-reduced ring B unsaturated estrogens. These results indicate that the ring B unsaturated estrogen Equilin is being metabolized in man in a somewhat similar manner to that of the classical estrogen estrone. Knowledge of the formation of 17 beta-dihydroequilin from Equilin in man is of importance because this estrogen is approximately 8 times more potent as a uterotrophic agent than the commonly used estrogen, Equilin.