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].
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.
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.
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].
Cymipristone, a progesterone receptor antagonist, is used potentially for termination of intrauterine pregnancy.
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].
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 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].
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].
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].
Progesterone is a steroid hormone that regulates the menstrual cycle and is crucial for pregnancy.
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].
Nestoron(ST1435; Elcometrine) is a 19-norprogesterone derivative and steroidal progestin which is used as a hormonal contraceptive; a high-affinity agonist of the progesterone receptor. IC50 value:Tareget: progesterone receptorNestorone acts primarily as a high-affinity agonist of the progesterone receptor. It lacks significant affinity for the androgen receptor, and accordingly, does not produce any androgenic or anabolic effects. It does not bind to the estrogen receptor either. Nestorone does however have some affinity for the glucocorticoid receptor, where it appears to act as an agonist, but it does not appear to produce any glucocorticoid side effects unless used at high doses. Nestorone does not bind to sex hormone-binding globulin, and is instead bound to serum albumin.
Drospirenone(Dihydrospirorenone) is a synthetic progestin that is an analog to spironolactone.Target: Progesterone ReceptorDrospirenone is a novel progestin under clinical development that is similar to the natural hormone progesterone, combining potent progestogenic with antimineralocorticoid and antiandrogenic activities. drospirenone was devoid of glucocorticoid activity. Both progestins did not show any antiglucocorticoid action. Furthermore, drospirenone and progesterone both showed considerable antimineralocorticoid activity and weak mineralocorticoid activity [1]. the pharmacological profile of drospirenone is more closely related to that of the natural hormone progesterone than is that of any other synthetic progestogen in use today. Therefore, drospirenone is anticipated to give rise to a number of additional health benefits both for users of oral contraceptives and hormone replacement therapy recipients [2]. The combination of 17beta-estradiol and drospirenone has a positive effect on BMD and a potentially beneficial effect on lipids. Although endometrial thickness increased slightly, the safety of the endometrium was assured, as no cases of hyperplasia or cancer occurred [3].Clinical indications: Acne; Dysmenorrhea; Endometriosis; Female contraception; Folic acid deficiency; Premenstrual syndrome
Tibolone is a broad spectrum gonadal steroid agonist with progestagenic, androgenic, and estrogenic activities. Tibolone can be used for postmenopausal osteoporosis research[1][2].
Gestodene(SHB 331;WL 70) is a progestogen hormonal contraceptive.Target: Estrogen Receptor/ERRGestodene is androgenically neutral, meaning that contraceptive pills containing gestodene do not exhibit the androgenic side effects (e.g. acne, hirsutism, weight gain) often associated with second-generation contraceptive pills, such as those containing levonorgestrel. When 40 micrograms of gestodene was taken, six out of seven women did not ovulate, and one out of seven had a cycle with luteal insufficiency. These data indicate that 40 micrograms of gestodene is the borderline dose for inhibition of ovulation. A combination of 75 micrograms gestodene with 30 micrograms ethinyl estradiol was found to inhibit ovulation in ten subjects, and no follicular maturation was noted [1]. gestodene bound with high affinity to the progesterone receptor, as did other synthetic and natural progestogens. However, gestodene did not bind to the estradiol receptor. The relative binding affinities of all tested synthetic and natural ligands showed no organ-specific differences and no differences between neoplastically transformed and normal tissues [2].Clinical indications: Female contraception
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].
Levonorgestrel is a synthetic progestogen used as an active ingredient in some hormonal contraceptives.Target: Progesterone ReceptorA synthetic progestational hormone with actions similar to those of progesterone and about twice as potent as its racemic or (+-)-isomer (norgestrel). It is used for contraception, control of menstrual disorders, and treatment of endometriosis. It is usually supplied in a racemic mixture (Norgestrel, 6533-00-2). Only the levonorgestrel isomer is active. Levonorgestrel is marketed mostly as a combination oral contraceptive under several brand names such as Alesse, Triphasil, and Min-Ovral [1].
Altrenogest(A35957; RU2267) is a progestogen structurally related to veterinary steroid trenbolone.Target: Progesterone ReceptorAltrenogest is a progestogen structurally related to veterinary steroid trenbolone. Treatment of embryo-recipient mares with altrenogest appears to be beneficial in extending the degree of donor-recipient synchrony required for successful embryo transfer. Altrenogest treatment also seems to be conductive to pregnancy maintenance in recipients experiencing luteal dysfunction [1]. The oil and gel altrenogest preparations are equally effective in modulating estrous behavior and time to estrus and ovulation. Altrenogest treatment started late in diestrus appears to result in a high incidence of ovulation during treatment and when luteolysis and ovulation occur during treatment; the subsequent luteal phase is frequently prolonged due to failure of regression of the CL [2].