ChemicalBook CAS DataBase List 7759-35-5

7759-35-5

Name	Nestoron
CAS	7759-35-5
Molecular Formula	C23H30O4
MDL Number	MFCD01711303
Molecular Weight	370.48
MOL File	7759-35-5.mol

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

Chemical Properties

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

Safety Data

Symbol(GHS)	GHS08
Signal word	Warning
Hazard statements	H351-H361
Precautionary statements	P201-P202-P281-P308+P313-P405-P501-P201-P202-P281-P308+P313-P405-P501
WGK Germany	3

Hazard Information

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 C_max in the blood and plasma are 58.1 and 95.5 ng equiv. ³H Nestoron/g, with t_1/2 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 (C_max) in the blood and plasma were 58.1 and 95.5 ng equiv./g, with t_1/2 of 15.6 hours. Approximately, 81.4% and 7.62% of the administered dose was excreted via feces and urine, respectively.

Spectrum Detail

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