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Nestoron

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Nestoron Basic information

Product Name:
Nestoron
Synonyms:
  • ST 1435
  • NESTORONE
  • NESTORON
  • 17-Hydroxy-16-methylene-19-norpregn-4-ene-3,20-dione acetate
  • Elcometrine
  • 17-(ACETYLOXY)-16-METHYLENE-19-NORPREGN-4-ENE-20-DIONE
  • 16-Methylene-17-hydroxy-19-norpregn-4-ene-3,20-dione acetate
  • 16-Methylene-17-alpha-acetoxy-19-nor-4-pregnene-3,20-dione
CAS:
7759-35-5
MF:
C23H30O4
MW:
370.48
Product Categories:
  • API
Mol File:
7759-35-5.mol
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Nestoron 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
InChI
InChI=1S/C23H30O4/c1-13-11-21-20-7-5-16-12-17(26)6-8-18(16)19(20)9-10-22(21,4)23(13,14(2)24)27-15(3)25/h12,18-21H,1,5-11H2,2-4H3/t18-,19+,20+,21-,22-,23-/m0/s1
InChIKey
CKFBRGLGTWAVLG-GOMYTPFNSA-N
SMILES
C1(=O)C=C2[C@]([H])(CC1)[C@]1([H])[C@]([H])([C@@]3([H])[C@@](CC1)(C)[C@@](OC(C)=O)(C(=O)C)C(=C)C3)CC2
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Safety Information

WGK Germany 
3
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Nestoron Usage And Synthesis

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.

NestoronSupplier

GUANGZHOU TOPWORK CHEMISTRY CO.,LTD. Gold
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Shanghai Boyle Chemical Co., Ltd.
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021-50182298 021-50180596
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025-83697070
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86-0571-85151182
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