Estrogen Receptor/ERR Antagonist

Estrogen Receptor/ERR Antagonists (67):

Cat. No.	Product Name	Effect	Purity

HY-13636

Fulvestrant	Antagonist	99.95%
Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC₅₀ of 9.4 nM. Fulvestrant is also a GPR30 agonist. Fulvestrant effectively inhibits the growth of ER-positive MCF-7 cells with an IC₅₀ of 0.29 nM. Fulvestrant also induces autophagy and has antitumor efficacy.

HY-103449

G15	Antagonist	≥99.0%
G15 is a high affinity and selective G-protein-coupled estrogen receptor (GPER/GPR30) antagonist with a K_i of 20 nM.

HY-103456

PHTPP	Antagonist	99.70%
PHTPP is a selective estrogen receptor β (ERβ) antagonist with 36-fold selectivity over ERα.

HY-13738A

Raloxifene hydrochloride	Antagonist	99.78%
Raloxifene hydrochloride (Keoxifene hydrochloride) is a second generation selective and orally active estrogen receptor modulator. Raloxifene hydrochloride produces estrogen-agonistic effects on bone and lipid metabolism and estrogen-antagonistic effects on uterine endometrium and breast tissue.

HY-10426

XCT790	Antagonist	99.54%
XCT-790 is a potent and selective inverse agonist for ERRα with an IC₅₀ value of 0.37 μM. XCT-790 induces cell death in chemotherapeutic resistant cancer cells. XCT-790 (Compound 12) is inactive against ERRγ and the estrogen receptors ERα and ERβ.

HY-12870

AZD9496	Antagonist	99.40%
AZD9496 is a potent and selective estrogen receptor (ERα) antagonist with an IC₅₀ of 0.28 nM. AZD9496 is an orally bioavailable selective oestrogen receptor degrader (SERD).

HY-109176

Giredestrant	Antagonist	99.52%
Giredestrant (GDC-9545), a non-steroidal estrogen receptor (ER) ligand, is an orally active and selective ER antagonist. Giredestrant potently competes with Estradiol for binding and induces a conformational change within the ER ligand binding domain. Giredestrant has anti-tumor activity.

HY-133017

Amcenestrant	Antagonist	99.59%
SAR439859 (compound 43d) is an orally active, nonsteroidal and selective estrogen receptor degrader (SERD). SAR439859 is a potent ER antagonist and has ER degrading activity with an EC₅₀ of 0.2 nM for ERα degradation. SAR439859 demonstrates robust antitumor efficacy and limited cross-resistance in ER⁺ breast cancer.

HY-113960

ERRα antagonist-1	Antagonist	99.71%
ERRα antagonist-1 (Compound A) is a selective and high affinity estrogen-related receptor α (ERRα) antagonist. ERRα antagonist-1 inhibits interaction of ERRα with Proliferator-activated Receptor γ Coactivator-1α (PGC-1α) and PGC-1β, the IC₅₀ values are 170 nM and 180 nM, respectively. ERRα antagonist-1 does not inhibit the interaction of either ERRβ or ERRγ with PGC-1α and PGC-1β coactivator, and also does not inhibit interaction of ERα or ERβ with PGC-1α or SRC-1.

HY-103450

G36	Antagonist	99.66%
G-36 is a cell permeable non-steroidal antagonist of G-protein-coupled estrogen receptor (GPER/GPR30) which selectively inhibits estrogen-mediated activation of PI3K by GPER, but not by ERα. G-36 also inhibits estrogen-mediated calcium mobilization (IC₅₀=112 nM).

HY-112596

H3B-6545	Antagonist	≥99.0%
H3B-6545 is an oral, selective estrogen receptor covalent antagonist (SERCA) for the research of metastatic ER-positive, HER2-negative breast cancer.

HY-118861A

Enclomiphene citrate	Antagonist	99.96%
Enclomiphene ((E)-Clomiphene) citrate is a potent and orally active non-steroidal estrogen receptor antagonist, with antioestrogenic property. Enclomiphene citrate can be used for the research of ovarian dysfunction, testosterone deficiency, male hypogonadism and type 2 diabetes.

HY-129099A

N-Desmethyltamoxifen hydrochloride	Antagonist	99.93%
N-Desmethyltamoxifen hydrochloride is the major metabolite of tamoxifen in humans. N-Desmethyltamoxifen, a poor antiestrogen, is a ten-fold more potent protein kinase C (PKC) inhibitor than Tamoxifen. N-Desmethyltamoxifen hydrochloride is also a potent regulator of ceramide metabolism in human AML cells, limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation.

HY-12870A

AZD9496 maleate	Antagonist
AZD9496 maleate is a potent and selective estrogen receptor (ERα) antagonist with IC₅₀ of 0.28 nM. AZD9496 maleate is an orally bioavailable selective oestrogen receptor degrader (SERD).

HY-U00425

PROTAC ERRα ligand 1	Antagonist	98.12%
PROTAC ERRα ligand 1 is an estrogen-related receptor α (ERRα) antagonist with IC₅₀s of 0.04 and 2.8 μM for ERRα and ERRγ, respectively.

HY-111484

GDC-0927	Antagonist	99.98%
GDC-0927 (SRN-927) is a potent, non-steroidal, orally bioavailable, selective estrogen receptor antagonist.

HY-145341

GNE-149	Antagonist	99.66%
GNE-149 is an orally bioavailable full antagonist of estrogen receptor α (ERα; IC₅₀=0.053 nM). GNE-149 is a selective estrogen receptor degrader (SERD). GNE-149 can be used for the research of breast cancer.

HY-126351

PROTAC ERRα ligand 2	Antagonist	99.75%
PROTAC ERRα ligand 2 is an estrogen-related receptor α (ERRα) inverse agonist with an IC₅₀ of 5.67 nM. PROTAC ERRα ligand 2 (IC₅₀=5.67 nM) displays a ~11-fold improved potency than XCT790 (IC₅₀=61.3 nM).

HY-16023

Acolbifene hydrochloride	Antagonist	99.00%
Acolbifene (EM-652) hydrochloride, an active metabolite of EM800, is an orally active, cancer-preventing selective estrogen receptor modulator (SERM). Acolbifene (EM-652) hydrochloride inhibits estradiol (E2)-induced transcriptional activity of ERα (IC₅₀=2 nM) and ERβ (IC₅₀=0.4 nM). Acolbifene (EM-652) hydrochloride exerts a potent and pure antiestrogenic action in the mammary gland and uterus. Anticarcinogenic properties.

HY-B0845

Prochloraz	Antagonist	99.77%
Prochloraz is an imidazole antifungal. Prochloraz is as an estrogen receptor (ER) and androgen receptor (AR) antagonist and an aromatase inhibitor with IC₅₀ values of 25 μM, 4 μM and 0.3 μM, respectively. Prochloraz is able to activate the aryl hydrocarbon receptor (AhR) having an EC₅₀ of 1 μM.

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