Nestoron

Modify Date: 2024-01-08 14:55:31

Nestoron Structure
Nestoron structure
Common Name Nestoron
CAS Number 7759-35-5 Molecular Weight 370.48200
Density 1.15g/cm3 Boiling Point 499.3ºC at 760mmHg
Molecular Formula C23H30O4 Melting Point N/A
MSDS Chinese USA Flash Point 216.2ºC

 Use of Nestoron


Nestoron(ST1435; Elcometrine) is a 19-norprogesterone derivative and steroidal progestin which is used as a hormonal contraceptive; a high-affinity agonist of the progesterone receptor. IC50 value:Tareget: progesterone receptorNestorone acts primarily as a high-affinity agonist of the progesterone receptor. It lacks significant affinity for the androgen receptor, and accordingly, does not produce any androgenic or anabolic effects. It does not bind to the estrogen receptor either. Nestorone does however have some affinity for the glucocorticoid receptor, where it appears to act as an agonist, but it does not appear to produce any glucocorticoid side effects unless used at high doses. Nestorone does not bind to sex hormone-binding globulin, and is instead bound to serum albumin.

 Names

Name Nestoron
Synonym More Synonyms

 Nestoron Biological Activity

Description Nestoron(ST1435; Elcometrine) is a 19-norprogesterone derivative and steroidal progestin which is used as a hormonal contraceptive; a high-affinity agonist of the progesterone receptor. IC50 value:Tareget: progesterone receptorNestorone acts primarily as a high-affinity agonist of the progesterone receptor. It lacks significant affinity for the androgen receptor, and accordingly, does not produce any androgenic or anabolic effects. It does not bind to the estrogen receptor either. Nestorone does however have some affinity for the glucocorticoid receptor, where it appears to act as an agonist, but it does not appear to produce any glucocorticoid side effects unless used at high doses. Nestorone does not bind to sex hormone-binding globulin, and is instead bound to serum albumin.
Related Catalog
References

[1]. Ilani N, et al. A New Combination of Testosterone and Nestorone Transdermal Gels for Male Hormonal Contraception.J Clin Endocrinol Metab. 2012 Jul 12.

[2]. Rad M, et al. Discriminant analysis of the metabolic effects of a new combined contraceptive vaginal ring containing Nestorone/EE vs. a second-generation oral contraceptive containing levonorgestrel/EE.Contraception. 2012 Sep;86(3):231-7. Epub 2012 Mar 23

[3]. Hussain R, et al. Progesterone and Nestorone facilitate axon remyelination: a role for progesterone receptors.Endocrinology. 2011 Oct;152(10):3820-31. Epub 2011 Aug 9.

[4]. Prasad PV, et al. Single-dose pharmacokinetics of Nestorone, a potential female-contraceptive.Steroids. 2010 Mar;75(3):252-64. Epub 2010 Jan 11.

[5]. Elsimar M Coutinho et al. Use of a single implant of elcometrine (ST-1435), a nonorally active progestin, as a long acting contraceptive for postpartum nursing women Contraception Volume 59, Issue 2, February 1999, Pages 115-122

 Chemical & Physical Properties

Density 1.15g/cm3
Boiling Point 499.3ºC at 760mmHg
Molecular Formula C23H30O4
Molecular Weight 370.48200
Flash Point 216.2ºC
Exact Mass 370.21400
PSA 60.44000
LogP 4.18520
Index of Refraction 1.549
Storage condition 2-8℃

 Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
RC8960750
CHEMICAL NAME :
19-Norpregn-4-ene-3,20-dione, 17-hydroxy-16-methylene-, acetate
CAS REGISTRY NUMBER :
7759-35-5
LAST UPDATED :
199306
DATA ITEMS CITED :
4
MOLECULAR FORMULA :
C23-H30-O4
MOLECULAR WEIGHT :
370.53

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Administration onto the skin
DOSE :
240 ug/kg
SEX/DURATION :
female 24 day(s) pre-mating
TOXIC EFFECTS :
Reproductive - Maternal Effects - menstrual cycle changes or disorders
REFERENCE :
FESTAS Fertility and Sterility. (American Fertility Soc., 608 13th Ave. S, Birmingham, AL 35282) V.1- 1950- Volume(issue)/page/year: 58,680,1992
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Implant
DOSE :
800 ug/kg
SEX/DURATION :
female 56 week(s) pre-mating
TOXIC EFFECTS :
Reproductive - Fertility - other measures of fertility
REFERENCE :
CCPTAY Contraception. (Geron-X, Inc., POB 1108, Los Altos, CA 94022) V.1- 1970- Volume(issue)/page/year: 25,299,1982
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Implant
DOSE :
2200 ug/kg
SEX/DURATION :
female 43 week(s) pre-mating
TOXIC EFFECTS :
Reproductive - Maternal Effects - menstrual cycle changes or disorders Reproductive - Fertility - female fertility index (e.g. # females pregnant per # sperm positive females; # females pregnant per # females mated)
REFERENCE :
CCPTAY Contraception. (Geron-X, Inc., POB 1108, Los Altos, CA 94022) V.1- 1970- Volume(issue)/page/year: 18,411,1978
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Implant
DOSE :
700 ug/kg
SEX/DURATION :
female 26 week(s) pre-mating
TOXIC EFFECTS :
Reproductive - Maternal Effects - menstrual cycle changes or disorders
REFERENCE :
FESTAS Fertility and Sterility. (American Fertility Soc., 608 13th Ave. S, Birmingham, AL 35282) V.1- 1950- Volume(issue)/page/year: 36,737,1981

 Safety Information

RIDADR NONH for all modes of transport

 Articles23

More Articles
Nestorone: clinical applications for contraception and HRT.

Steroids 68(10-13) , 907-13, (2003)

The 19-nor derivatives of progesterone are referred to as "pure" progestational molecules as they bind almost exclusively to the progesterone receptor (PR) without interfering with receptors of other ...

Recent developments in contraceptive implants at the Population Council.

Contraception 65(1) , 113-9, (2002)

Development of contraceptive implant methods, when based on established or on new synthetic chemical entities, is a decadal or multi-decadal process. The process often requires the cooperation of nume...

Central modifications of allopregnanolone and beta-endorphin following subcutaneous administration of Nestorone.

J. Steroid Biochem. Mol. Biol. 116(1-2) , 15-20, (2009)

The aim of the present study was to evaluate the potential action of Nestorone (alone or in combination with estradiol valerate) on the level of allopregnanolone and of the opioid beta-endorphin in se...

 Synonyms

NESTORONE
19-Norpregn-4-ene-3,20-dione,17-hydroxy-16-methylene-,acetate
16-Methylene-17-hydroxy-19-norpregn-4-ene-3,20-dione acetate
17-(ACETYLOXY)-16-METHYLENE-19-NORPREGN-4-ENE-20-DIONE
17-Hydroxy-16-methylene-19-norpregn-4-ene-3,20-dione acetate
Elcometrine
Top Suppliers:I want be here
  • DC Chemicals Limited
  • China
  • Product Name: Nestorone
  • Price: $Inquiry/500mg $135.0/25mg $225.0/100mg
  • Purity: 98.0%
  • Stocking Period: 3 Day
  • Contact: Tony Cao


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Price: $79/10mM*1mLinDMSO

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