Nestoron - CAS 7759-35-5
Catalog number: 7759-35-5
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C23H30O4
Molecular Weight:
370.48
COA:
Inquire
Targets:
Progesterone Receptor
Description:
Nestorone is a steroidal progestin of the 19-norprogesterone group which is used as a hormonal contraceptive in several South American countries. It is a potent progesterone receptor agonist with no androgenic, estrogenic, or glucocorticoid-like activities. It has been used as a female contraceptive and may be useful as a male contraceptive too recently. It does not bind to the estrogen receptor either, but it has some affinity for the glucocorticoid recepto. It appears to act as an agonist, but it does not appear to produce any glucocorticoid side effects unless used at high doses. It has been shown to have neurogenic and neuroprotective activity. It holds back proinflammatory mediators and neuropathology in the wobbler mouse model of motoneuron degeneration. It protected against hippocampus abnormalities and improved functional outcomes of EAE mice, which suggests its potential value. It lacks affinity for the androgen receptor, thus does not produce any androgenic or anabolic effects. It is being in Clinical stage 1.
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Purity:
95%
Appearance:
White to beige powder
Synonyms:
ST 1435;17-Hydroxy-16-methylene-19-norpregn-4-ene-3,20-dione acetate;Elcometrine;16-Methylene-17-hydroxy-19-norpregn-4-ene-3,20-dione acetate;Segesterone acetate;[(8R,9S,10R,13S,14S,17R)-17-acetyl-13-methyl-16-methylidene-3-oxo-2,6,7,8,9,10,11,12,14,15-decahydro-1H-cyclopenta[a]phenanthren-17-yl] acetate
Solubility:
10 mM in DMSO
Storage:
-20°C Freezer
MSDS:
Inquire
Application:
Nestorone is used as a hormonal contraceptive in several South American countries. It has been used as a female contraceptive and may be useful as a male contraceptive too recently. It lacks affinity for the androgen receptor, thus does not produce any androgenic or anabolic effects.
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Grams to Kilograms
Boiling Point:
499.3±45.0 °C | Condition: Press: 760 Torr
Density:
1.15±0.1 g/cm3 | Condition: Temp: 20 °C Press: 760 Torr
InChIKey:
CKFBRGLGTWAVLG-GOMYTPFNSA-N
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
Canonical SMILES:
CC(=O)C1(C(=C)CC2C1(CCC3C2CCC4=CC(=O)CCC34)C)OC(=O)C
Current Developer:
Being in Clinical stage 1. Several Chinese companies or research institutions are developing the product, such as China Medicine University, Xianju Zhejiang pharmaceutical and so on.
1.Efficacy of the selective progesterone receptor agonist Nestorone for chronic experimental autoimmune encephalomyelitis.
Garay L1, Gonzalez Deniselle MC2, Sitruk-Ware R3, Guennoun R4, Schumacher M4, De Nicola AF5. J Neuroimmunol. 2014 Nov 15;276(1-2):89-97. doi: 10.1016/j.jneuroim.2014.08.619. Epub 2014 Aug 28.
Progesterone plays a protective role in the experimental autoimmune encephalomyelitis (EAE) model of multiple sclerosis (MS). Besides spinal cord neuropathology, MS patients present a dysfunctional hippocampus. In this work we studied the therapeutic effects of the progestin Nestorone in the brain of mice with chronic EAE. Nestorone decreased clinical grade and enhanced motor behavior. In addition, it increased cell proliferation and doublecortin positive neuroblasts in the hippocampus, increased GABAergic interneurons and attenuated the number of Iba1+ microglia/macrophages, events possibly linked to enhancement of neurogenesis. Therefore, Nestorone protected against hippocampus abnormalities and improved functional outcomes of EAE mice, suggesting its potential value for MS.
2.Progesterone and nestorone promote myelin regeneration in chronic demyelinating lesions of corpus callosum and cerebral cortex.
El-Etr M1, Rame M, Boucher C, Ghoumari AM, Kumar N, Liere P, Pianos A, Schumacher M, Sitruk-Ware R. Glia. 2015 Jan;63(1):104-17. doi: 10.1002/glia.22736. Epub 2014 Aug 4.
Multiple Sclerosis affects mainly women and consists in intermittent or chronic damages to the myelin sheaths, focal inflammation, and axonal degeneration. Current therapies are limited to immunomodulators and antiinflammatory drugs, but there is no efficient treatment for stimulating the endogenous capacity of myelin repair. Progesterone and synthetic progestins have been shown in animal models of demyelination to attenuate myelin loss, reduce clinical symptoms severity, modulate inflammatory responses and partially reverse the age-dependent decline in remyelination. Moreover, progesterone has been demonstrated to promote myelin formation in organotypic cultures of cerebellar slices. In the present study, we show that progesterone and the synthetic 19-nor-progesterone derivative Nestorone® promote the repair of severe chronic demyelinating lesions induced by feeding cuprizone to female mice for up to 12 weeks. Progesterone and Nestorone increase the density of NG2(+) oligodendrocyte progenitor cells and CA II(+) mature oligodendrocytes and enhance the formation of myelin basic protein (MBP)- and proteolipid protein (PLP)-immunoreactive myelin.
3.[The "pill" for him remains a long-term pious aspiration].
Müller T. MMW Fortschr Med. 2015 Nov 12;157 Spec No 2:18.
4.Acceptability of the Nestorone®/ethinyl estradiol contraceptive vaginal ring: development of a model; implications for introduction.
Merkatz RB1, Plagianos M2, Hoskin E2, Cooney M2, Hewett PC3, Mensch BS2. Contraception. 2014 Nov;90(5):514-21. doi: 10.1016/j.contraception.2014.05.015. Epub 2014 Jun 2.
OBJECTIVES: Develop and test a theoretical acceptability model for the Nestorone®/ethinyl estradiol contraceptive vaginal ring (CVR); explore whether domains of use within the model predict satisfaction, method adherence and CVR continuation.
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CAS 7759-35-5 Nestoron

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