A synthetic progestogen
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Megestryl Acetate

Item No. 21749

Technical Information
Formal Name
17-(acetyloxy)-6-methyl-pregna-4,6-diene-3,20-dione
CAS Number
595-33-5
Synonyms
  • Megestrol Acetate
  • NSC 71423
  • SC-10363
Molecular Formula
C24H32O4
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
λmax
288 nm
SMILES
CC1=C[C@]([C@@](CC[C@]2(OC(C)=O)C(C)=O)([H])[C@]2(C)CC3)([H])[C@@]3([H])[C@]4(C)C1=CC(CC4)=O
InChi Code
InChI=1S/C24H32O4/c1-14-12-18-19(22(4)9-6-17(27)13-21(14)22)7-10-23(5)20(18)8-11-24(23,15(2)25)28-16(3)26/h12-13,18-20H,6-11H2,1-5H3/t18-,19+,20+,22-,23+,24+/m1/s1
InChi Key
RQZAXGRLVPAYTJ-GQFGMJRRSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Megestryl acetate is a synthetic progestogen and derivative of progesterone originally developed as a contraceptive.1 It binds with high relative affinity to the progesterone (Item No. 15876), androgen, and glucocorticoid receptors in mammary cancer cells.2 It increases neuropeptide Y (Item No. 15071) by 90-140% and inhibits calcium channel currents in the rat hypothalamus.3,4 Megestryl acetate decreases cytokine and serotonin production in patient-derived peripheral blood mononuclear cells (PBMCs).5 In rats, it increases food and water intake when administered at a dose of 50 mg/kg per day.3 Formulations containing megestryl acetate have been used in the treatment of endometriosis, hormone-related cancers, and as an appetite stimulant for cancer patients with anorexia and cachexia.6

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Østergaard, M.D. The oral progestational and anti-ovulatory properties of megestrol acetate and its therapeutic use in gynaecological disorders. J. Obstet. Gynaecol. Br. Emp. 72(1), 45-48 (1965).

    2. Teulings, F.A., van Glise, H.A., Henkelman, M.S., et alEstrogen, androgen, glucocorticoid, and progesterone receptors in progestin-induced regression of human breast cancer. Cancer Res. 40(7), 2557-2561 (1980).

    3. McCarthy, H.D., Crowder, R.E., Dryden, S., et alMegestrol acetate stimulates food and water intake in the rat: Effects on regional hypothalamic neuropeptide Y concentrations. Eur. J. Pharmacol. 265(1-2), 99-102 (1994).

    4. Costa, A.-M., Spence, K.T., Plata-Salamán, C.R., et alResidual Ca2+ channel current modulation by megestrol acetate via a G-protein αs-subunit in rat hypothalamic neurones. J. Physiol. 487(Pt 2), 291-303 (1995).

    5. Mantovani, G., Macciò, A., Esu, S., et alMedroxyprogesterone acetate reduces the in vitro production of cytokines and serotonin involved in anorexia/cachexia and emesis by peripheral blood mononuclear cells of cancer patients. Eur. J. Cancer 33(4), 602-607 (1997).

    6. Argilés, J.M., Anguera, A., and Stemmler, B. A new look at an old drug for the treatment of cancer cachexia: Megestrol acetate. Clin. Nutr. 32(3), 319-324 (2013).