| Identification | Back Directory | [Name]
Nestoron | [CAS]
7759-35-5 | [Synonyms]
ST 1435
NESTORON
NESTORONE
Elcometrine
Nestoron (ST-1435)
Segesterone Acetate
ELCOMETRINE;NESTORONE;ST-1435;ST1435
ELCOMETRINE; NESTORONE; ST-1435; ST 1435; ST1435
17-(ACETYLOXY)-16-METHYLENE-19-NORPREGN-4-ENE-20-DIONE
17-(Acetyloxy)-16-methylene-19-norpregn-4-ene-3,20-dione
19-Norpregn-4-ene-3,20-dione, 17-(acetyloxy)-16-methylene-
16-Methylene-17-alpha-acetoxy-19-nor-4-pregnene-3,20-dione
16-Methylene-17-hydroxy-19-norpregn-4-ene-3,20-dione acetate
17-Hydroxy-16-methylene-19-norpregn-4-ene-3,20-dione acetate
Estr-4-en-3-one,17-acetyl-17-(acetyloxy)-16-methylene-,(17α)-
19-Norpregn-4-ene-3,20-dione, 17-hydroxy-16-methylene-, acetate
19-Norpregn-4-ene-3,20-dione, 17-(acetyloxy)-16-methylene- (9ci)
(8R,9S,10R,13S,14S,17R)-17-acetyl-13-methyl-16-methylene-3-oxo-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl acetate | [Molecular Formula]
C23H30O4 | [MDL Number]
MFCD01711303 | [MOL File]
7759-35-5.mol | [Molecular Weight]
370.48 |
| Chemical Properties | Back Directory | [Melting point ]
178-179° | [alpha ]
D21 -105° (c = 1.2 in chloroform) | [Boiling point ]
420.37°C (rough estimate) | [density ]
1.0550 (rough estimate) | [refractive index ]
1.4433 (estimate) | [storage temp. ]
2-8°C | [solubility ]
DMSO: soluble5mg/mL, clear | [form ]
powder | [color ]
white to beige | [InChIKey]
CKFBRGLGTWAVLG-GOMYTPFNSA-N |
| Hazard Information | Back Directory | [Uses]
Segesterone Acetate has been used to study the: comparison of androgenic and estrogenic properties of progestins used in contraception and hormone therapy; impact on hepatic estrogen-sensitive proteins by 1-yr contraceptive vaginal ring delivering Nestorone and ethinyl estradiol. | [Definition]
ChEBI: Elcometrine is a corticosteroid hormone. | [Pharmacokinetics]
Elcometrine is a member of the 19-norprogesterone class of pr ogestins. when administered subcuta neously (implant), intravaginally (vaginal ring), or transdermally, elcometrine is an exceptionally potent progestin. It is 100-fold more potent when administered subcutaneously than when delivered orally. Its oral bioavaiability is only 10%，with a half life of just 1 to 2 hours because of rapid metabolism. The C16 methylene functionality substantially increases its affinity for the progesterone receptor. | [Clinical Use]
Because of its antiestrogenic action, elcometrine also can be administered transdermally along with estradiol as a treatment for menopausal symptoms . | [in vivo]
Nestoron (400 μCi 3H Nestoron/kg BW; subcutaneous injection; female Sprague-Dawley rats) treatment results in the Cmax in the blood and plasma are 58.1 and 95.5 ng equiv. 3H Nestoron/g, with t1/2 of 15.6 hours. Approximately, 81.4% and 7.62% of the administered dose is excreted via feces and urine, respectively[1]. | Animal Model: | 27 adult, female, Sprague-Dawley rats (200-225 g; age: 8 weeks)[1] | | Dosage: | 400 μCi 3H Nestorone/kg BW | | Administration: | Subcutaneous injection (Pharmacokinetic study) | | Result: | The mean peak concentrations of radioactivity (Cmax) in the blood and plasma were 58.1 and 95.5 ng equiv./g, with t1/2 of 15.6 hours. Approximately, 81.4% and 7.62% of the administered dose was excreted via feces and urine, respectively.
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