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Nomegestrol acetate

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Nomegestrol acetate is a progestin compound used as a drug substance in pharmaceutical applications. It is a synthetic derivative of the naturally occurring hormone progesterone. The core function of nomegestrol acetate is to provide progestogenic activity in hormonal therapies.

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Lab products found in correlation

Levonorgestrel, by Merck Group (2 mentions) Nestorone, by Merck Group (2 mentions) Gestodene, by Merck Group (2 mentions) Drospirenone, by Merck Group (2 mentions) Leupeptin, by Carl Roth (2 mentions) Aprotinin, by Carl Roth (2 mentions) Pepstatin, by Carl Roth (2 mentions) Pefabloc, by Carl Roth (2 mentions) Dimethyl sulfoxide (dmso), by Merck Group (2 mentions) Dihydrotestosterone, by Merck Group (1 mentions) Fulvestrant ici182 780, by Merck Group (1 mentions) Net a, by Merck Group (1 mentions) Phorbol 12 myristate 13 acetate pma, by Merck Group (1 mentions) Medroxyprogesterone acetate, by Merck Group (1 mentions) Norethisterone, by Merck Group (1 mentions) Phorbol myristate acetate (pma), by Merck Group (1 mentions) R5020, by PerkinElmer (1 mentions) Doxorubicin, by Merck Group (1 mentions) 1 chloro 2 4 dinitrobenzene cdnb, by Merck Group (1 mentions) β glucuronidase from bovine liver, by Merck Group (1 mentions)

4 protocols using nomegestrol acetate

1

Receptor Binding Assay Protocol

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P4, MPA, NET-A, levonorgestrel (LNG), gestodene (GES), nestorone (NES), nomegestrol acetate (NoMAC), drospirenone (DRSP), dihydrotestosterone (DHT), hydroxyflutamide (OHF), estradiol (E2), fulvestrant (ICI 182,780) and phorbol 12-myristate13-acetate (PMA) were obtained from Sigma-Aldrich, RSA. Human tumor necrosis factor-alpha (TNFα) was obtained from Celtic Diagnostics, RSA. Unlabeled mibolerone (MIB) and [3H]-MIB (84.3 Ci/mmol) were purchased from PerkinElmer Life and Analytical Science, RSA, while [3H]-E2 (100 Ci/mmol) was obtained from AEC-Amersham, RSA.
Louw-du Toit R., Perkins M.S., Hapgood J.P, & Africander D. (2017). Comparing the androgenic and estrogenic properties of progestins used in contraception and hormone therapy. Biochemical and biophysical research communications, 491(1), 140-146.
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2

Breast Cancer Cell Line Maintenance

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The human MDA-MB-231 breast cancer cell line was gifted by Prof. Adrienne Edkins (Rhodes University, RSA) and was maintained as previously described in [12 (link)], with only mycoplasma negative cells used in experiments. R5020 was purchased from Perkin Elmer Life and Analytical Science, while P4, medroxyprogesterone acetate (MPA), norethisterone (NET), levonorgestrel (LNG), gestodene (GES), nestorone (NES), nomegestrol acetate (NOMAC), drospirenone (DRSP), and phorbol myristate acetate (PMA) were purchased from Sigma-Aldrich. The human PR-A expression vector (pSG5-hPR-A) [13 (link)] and the pSG5-empty expression vector containing no eukaryotic promoter or enhancer sequences [14 (link)] were received from Dr. Eric Kalkhoven (University Medical Centre, Utrecht, Netherlands) and Prof. Gunnar Mellgren (University of Bergen, Norway), respectively. The pTAT-2x-progesterone response element (PRE)-E1b-luciferase promoter-reporter construct [15 (link)] was received from Prof. Guido Jenster (Erasmus University of Rotterdam, Netherlands), while the 5x-nuclear factor kappa beta (NFκB)-luciferase promoter-reporter construct was purchased from Stratagene (Houston, Texas).
Cartwright M., Toit R.L, & Africander D. (2022). The transcriptional activity of progestins used in contraception and menopausal hormone therapy via progesterone receptor A is dependent on the density of the receptor. Biochemical and biophysical research communications, 639, 70-76.
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3

Cytotoxicity Assay with CDNB

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Cell culture media, fetal bovine serum, L-glutamine, penicillin and streptomycin, non-essential amino acids, 1-chloro-2,4-dinitrobenzene (CDNB), 5(6)-carboxy-2′,7′-dichlorofluorescein diacetate (CDFDA), Hank's buffered saline solution (HBSS), doxorubicin, 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT), β-glucuronidase from bovine liver, MK571, nomegestrol acetate (NMGA) and sulfatase from Helix pomatia type H-1 were from Sigma-Aldrich (St. Louis, USA). Aprotinin, leupeptin, pepstatin and pefabloc were from Carl Roth (Karlsruhe, Germany). DMSO was from Merck (Darmstadt, Germany). The glutathione-conjugated derivative of CDNB, 2,4-dinitrophenyl-S-glutathione (DNP-SG), was synthesized with the use of 1fluoro-2,4-dinitrobenzene and glutathione as described by Sokolovsky et al. (1964) (link). All other chemicals were of analytical grade purity or higher.
Tocchetti G.N., Domínguez C.J., Zecchinati F., Arana M.R., Ruiz M.L., Villanueva S.S.M., Mottino A.D., Weiss J, & Rigalli J.P. (2018). Inhibition of multidrug resistance-associated protein 2 (MRP2) activity by the contraceptive nomegestrol acetate in HepG2 and Caco-2 cells. European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences, 122.
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4

Cell Culture Reagents and Inhibitors

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AG-205, nomegestrol acetate (NMGA), cell culture media and all supplements were from Sigma-Aldrich (St. Louis, USA). Ponceau S, ethanol, aprotinin, leupeptin, pepstatin and pefabloc were from Carl Roth (Karlsruhe, Germany). 3-isobutyl-1methylxanthine (IBMX), actinomycin D, calcein-AM, H-89 dihydrochloride (H89), KT5720, Rp-8-Br-cAMP, mifepristone (RU 486), PSC833, Ro 20-1724 and SC68376 were from Santa Cruz Biotechnology (Heidelberg, Germany). Bordetella pertussis toxin (PTX) was from Enzo Life Sciences (Farmingdale, USA). PD98059 was from Calbiochem (San Diego, USA). Polyvinylidene difluoride (PVDF) membranes were from GE Healthcare (Little Chalfont, UK). DharmaFECT4 Transfection Reagent was from Dharmacon (Lafayette, USA). DMSO was from Merck (Darmstadt, Germany).
All other chemicals were of analytical grade purity.
Tocchetti G.N., Domínguez C.J., Zecchinati F., Arana M.R., Ruiz M.L., Villanueva S.S.M., Weiss J., Mottino A.D, & Rigalli J.P. (2018). Biphasic modulation of cAMP levels by the contraceptive nomegestrol acetate. Impact on P-glycoprotein expression and activity in hepatic cells. Biochemical pharmacology, 154.
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