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Cat. No. Product Name CAS No. Information
PC-60063

Enclomiphene citrate

7599-79-3

Enclomiphene citrate((E)-Clomifene, cis-Clomifene, RMI-16289, ICI-46476) is a nonsteroidal selective estrogen receptor modulator (SERM) that is under development for the treatment of male hypogonadism; inhibits the ER in the pituitary gland, reduces negative feedback by estrogen on the hypothalamic-pituitary-gonadal axis, increases gonadotropin secretion and hence gonadal production of testosterone.

Sexual Dysfunction

Phase 3 Clinical

PC-45734

Elacestrant dihydrochloride

1349723-93-8

Elacestrant (RAD-1901) is a novel, orally bioavailable small-molecule selective estrogen receptor degrader (SERD); inhibits ERα expression in MCF-7 cells (IC50=0.6 nM); induces the degradation of ER, inhibits ER-mediated signaling and growth of ER+ breast cancer cell lines in vitro and in vivo, and significantly inhibits tumor growth of multiple PDX models.

Breast Cancer

Phase 2 Clinical

PC-45733

Elacestrant

722533-56-4

Elacestrant (RAD-1901) is a novel, orally bioavailable small-molecule selective estrogen receptor degrader (SERD); inhibits ERα expression in MCF-7 cells (IC50=0.6 nM); induces the degradation of ER, inhibits ER-mediated signaling and growth of ER+ breast cancer cell lines in vitro and in vivo, and significantly inhibits tumor growth of multiple PDX models.

Breast Cancer

Phase 2 Clinical

PC-43271

AZD9496 maleate

1639042-28-6

A potent, selective estrogen receptor downregulator (SERD) with ER downregulation pIC50 of 9.68; shows pM equipotent binding to both ERα and ERβ isoforms, highly selective binding compared with progesterone (∼650-fold), glucocorticoid (∼11,223-fold), and androgen (∼36,375-fold) receptor LBDs; downregulator of ERα in vitro and in vivo in ER-positive models of breast cancer and orally available.

Breast Cancer

Phase 1 Clinical

PC-43270

AZD9496

1639042-08-2

A potent, selective estrogen receptor downregulator (SERD) with ER downregulation pIC50 of 9.68; shows pM equipotent binding to both ERα and ERβ isoforms, highly selective binding compared with progesterone (∼650-fold), glucocorticoid (∼11,223-fold), and androgen (∼36,375-fold) receptor LBDs; downregulator of ERα in vitro and in vivo in ER-positive models of breast cancer and orally available.

Breast Cancer

Phase 1 Clinical

PC-42580

XCT790

725247-18-7

A potent and selective ERRα inverse agonist with IC50 of 300-500 nM in transient transfection assays; shows no significant antagonist activity on related nuclear receptors (ERRγ or ERα, LXRα, LXRβ, FXR, PPARα, PPARδ, PPARγ, Nurr1, RARα, RORα, and RXRα) at 10 uM; inhibits PGC-1α regulation of ERRα and ERRα target gene expression; inhibits proliferation in cellular models of breast cancer.

PC-46618

Clomiphene citrate

50-41-9

A non-steroidal, a widely used fertility agent that inhibits estrogen receptor in the hypothalamus; shows antibacterial activity by inhibiting undecaprenyl diphosphate synthase, an enzyme that catalyzes the synthesis of a polyisoprenoid essential for both peptidoglycan and wall teichoic acid (WTA) synthesis.

Other Indication

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