Ethynodiol diacetate is a steroidal progestin which is used as a hormonal contraceptive, it has relatively little or no potency as an androgen,has significant estrogenic effects.
Promegestone (R-5020), a progestin, is a potent progesterone receptor (PR) agonist. Promegestone has the potential for endocrine regulation and cancer research[1].
Norgestrienone, progestin or synthetic progestin, is a progestin receptor agonist. Norgestrienone is often used as a progestational compound in birth control pills and can be used in combination with ethinyl estradiol[1].
Chlormadinone acetate is a steroidal progestin, with antiandrogen and antiestrogenic effects.
Mifepristone is a progesterone receptor (PR) and glucocorticoid receptor (GR) antagonist with IC50s of 0.2 nM and 2.6 nM in in vitro assay.
Cymipristone, a progesterone receptor antagonist, is used potentially for termination of intrauterine pregnancy.
ARD-61 is a highly potent, effective and specific PROTAC androgen receptor (AR) degrader. ARD-61 potently and effectively induces AR and progesterone receptors (PR) degradation in AR+ cancer cell lines. ARD-61 induces apoptosis and effectively induces tumor growth inhibition in the MDA-MB-453 xenograft model in mice[1].
Desogestrel(Org-2969) is a third-generation 19-nortestosterone derivative progestogen; is contained in many oral contraceptive preparations, both combined (COCs) to ethinyl-estradiol (EE) or alone in a progestin-only pill (POP).
Nomegestrol acetate is a potent, highly selective progestogen, which is characterized as a full agonist at the progesterone receptor, with no or minimal binding to other steroid receptors, including the androgen and glucocorticoid receptors[1].
Estradiol dipropionate is a combined estrogen-progesterone, acts as an estrogen and progesterone agonist[1].
Ulipristal (acetate) is a novel selective progesterone receptor modulator (SPRM) for the treatment of benign gynecological conditions such as uterine myoma.
Trimegestone (RU 27987) is an orally active 19-norpregnane progestin. Trimegestone binds to progesterone receptor (PR) with an IC50 value of 3.3 nM (rat PR). Trimegestone increases alkaline phosphatase activity (EC50=0.1 nM) but not luciferase activity. Trimegestone also shows a weak antiandrogenic activity (weak androgen receptor affinity). Trimegestone can be used in studies of contraception or menopausal syndromes[1][2].
ZK112993 is a potent progesterone receptor (PR) antagonist. ZK112993 significantly inhibits the growth of T61 human tumors in nude mice[1].
Ulipristal (CDB 3236) is a selective progesterone receptor modulator (SPRM). Ulipristal binds to the progesteron receptor, thereby inhibiting PR-mediated gene expression, and interfering with progesterone activity in the reproductive system[1].
Dexamethasone oxetanone (Dex-Ox), a derivative of the glucocorticoid-selective steroid Dexamethasone (Dex), is an antiglucocorticoid. Dexamethasone oxetanone is an antiprogestin with significant agonist activity with progesterone receptor (PR) A and B isoforms[1][2].
Drospirenone-d4 (Dihydrospirorenone-d4) is the deuterium labeled Drospirenone. Drospirenone (Dihydrospirorenone) is a synthetic progestin that is an analog to spironolactone[1][2].
Megestrol Acetate is a synthetic progesteronal agent with an IC50 of 260 μM for the inhibition of HegG2.Target: Progesterone ReceptorMegestrol acetate, also known as 17α-acetoxy-6-dehydro-6-methylprogesterone, and sometimes abbreviated as MGA or MA, is a steroidal progestin and progesterone derivative (specifically, a 17-hydroxylated progesterone) with predominantly progestational and antigonadotropic effects. Megestrol acetate is a good candidate for muscle wasting treatment and future studies addressed at the interaction between the drug and protein turnover in human skeletal muscle should be performed.
Norethindrone acetate is a female progestin approved by FDA for the treatment of endometriosis, uterine bleeding caused by abnormal hormone levels, and secondary amenorrhea.
PF-3882845 is a remarkably high affinity selective and orally efficacious mineralocorticoid receptor (MR binding IC50=2.7 nM) antagonist for hypertension and nephropathy. PF-3882845 also binds to progesterone receptor (PR) with the binding IC50 of 310 nM[1].
Medroxyprogesterone is a progestin, a synthetic variant of the human hormone progesterone and a potent progesterone receptor agonist.Target: Progesterone ReceptorMedroxyprogesterone (MP), is a steroidal progestin drug which was never marketed for use in humans. An acylated derivative, medroxyprogesterone acetate (MPA), is clinically used as a pharmaceutical medicine. Compared to MPA, MP is over two orders of magnitude less potent as a progestogen. As such, MP itself is not used clinically, though it has seen limited use in veterinary medicine under the trade name Controlestril in France. In addition, it is an metabolite of MPA [1].
Ulipristal acetate-d6 is deuterium labeled Ulipristal acetate. Ulipristal acetate (CDB-2914) is an orally active, selective progesterone receptor modulator (SPRM). Ulipristal acetate stimulates the autophagic response selectively in leiomyoma cells. Ulipristal acetate has the potential for benign gynecological conditions treatment, such as uterine myoma[1][2].
Norethindrone-d6 is the deuterium labeled Norethindrone. Norethindrone is a female progestin approved by FDA for the treatment of endometriosis, uterine bleeding caused by abnormal hormone levels, and secondary amenorrhea.
Norethindrone is a female progestin approved by FDA for the treatment of endometriosis, uterine bleeding caused by abnormal hormone levels, and secondary amenorrhea.
Norethisterone enanthate is a long-acting parenteral progestogen. Norethisterone enanthate is orally active[1][2][3].
Melengestrol acetate is a progesterone derivative, acts as an orally active corticosteroid hormone to promote endometrial proliferation, pregnancy maintenance, and delay of menstrual activity[1]. Melengestrol Acetate is used as a contraceptive agent for growth promoting effects and suppression of estrus in animals. Melengestrol acetate inhibits both the androgen-dependent and -independent prostatic tumors in vivo and can be used for cancer research[2].
Cridanimod is a small-molecule immunomodulator and interferon inducer[1]. Cridanimod is a potent progesterone receptor (PR) activator mediated through induction of IFNα and IFNβ expression[2].
Norgestimate, a synthetic progesterone analog, is an orally active progestin with highly selective progestational activity and minimal androgenicity. Norgestimate is used for an oral contraceptive[1][2].
Nomegestrol is a potent and orally available progestin, acts as a selective full progesterone receptor agonist, with a Kd of 5.44 nM for rat uterine progesterone receptor, and has moderate antiandrogenic activity and strong antiestrogenic activity.
Asoprisnil (J867), a selective progesterone receptor modulator, exhibits mixed progesterone agonist and antagonist effects on various progesterone targeted tissues in animal and human[1].
Org OD 02-0 (10-Ethenyl-19-norprogesterone) is a membrane progesterone receptor α (mPRα)-specific agonist (IC50: 33.9 nM). Org OD 02-0 activates MAPK activity. Org OD 02-0 inhibits prolactin (PRL) secretion in the pituitary[1][2].