Nestoron

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Chemical Structure| 7759-35-5 同义名 : Elcometrine;ST-1435;Segesterone acetate
CAS号 : 7759-35-5
货号 : A503435
分子式 : C23H30O4
纯度 : 98%
分子量 : 370.482
MDL号 : MFCD01711303
存储条件：

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(94.47 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Nestoron is a 19-norprogesterone derivative with high affinity and selectivity for progesterone receptors. 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[3]. Nestorone® (NES) is a potent nonandrogenic progestin being developed for contraception. The neuroprotective and myelin regenerative effects of NES are mediated via PR (progesterone receptor) binding and not via its interaction with the GABAAR(γ-aminobutyric acid type A receptor)[4]. NES (Nestorone®) alone or with E2 (Estradiol) increased the levels of transcription factors, essential for myelin synthesis[5]. The increase in oligodendroglial cells by Nestorone resulted from enhanced NG2(+) and Olig2(+) oligodendrocyte progenitor cell (OPC) recruitment. Nestorone stimulated the migration of OPC towards demyelinated axons. In this coculture paradigm, Nestorone indeed markedly increased the number of EGFP(+) cells migrating into the demyelinated cerebellar slices[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.70mL

0.54mL

0.27mL

13.50mL

2.70mL

1.35mL

26.99mL

5.40mL

2.70mL
参考文献

[1]Ilani N, Roth MY, et al. A new combination of testosterone and nestorone transdermal gels for male hormonal contraception. J Clin Endocrinol Metab. 2012 Oct;97(10):3476-86.

[2]Rad M, Burggraaf J, 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.

[3]Prasad PV, Bashir M, Sitruk-Ware R, Kumar N. Single-dose pharmacokinetics of Nestorone, a potential female-contraceptive. Steroids. 2010 Mar;75(3):252-64

[4]Kumar N, Fagart J, Liere P, Mitchell SJ, Knibb AR, Petit-Topin I, Rame M, El-Etr M, Schumacher M, Lambert JJ, Rafestin-Oblin ME, Sitruk-Ware R. Nestorone® as a Novel Progestin for Nonoral Contraception: Structure-Activity Relationships and Brain Metabolism Studies. Endocrinology. 2017 Jan 1;158(1):170-182

[5]El-Etr M, Akwa Y, Rame M, Schumacher M, Sitruk-Ware R. Nestorone® , a 19nor-progesterone derivative boosts remyelination in an animal model of demyelination. CNS Neurosci Ther. 2021 Apr;27(4):464-469

[6]Hussain R, El-Etr M, Gaci O, Rakotomamonjy J, Macklin WB, Kumar N, Sitruk-Ware R, Schumacher M, Ghoumari AM. Progesterone and Nestorone facilitate axon remyelination: a role for progesterone receptors. Endocrinology. 2011 Oct;152(10):3820-31