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Home > Inhibitors & Agonists > Nuclear Receptor/Transcription Factor > Estrogen Receptor/ERR

PHTPP

  Cat. No.:  DC10846   Featured
Chemical Structure
805239-56-9
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Field of application
PHTPP is a pyrazolo[1,5-α]pyrimidine-based ligand that acts as a full antagonist of estrogen ERβ receptors with 36-fold selectivity over ERα.
Chemicals PropertiesBiological activity COAMSDSRelated productsDatasheet
Cas No.: 805239-56-9
Chemical Name: 4-[2-phenyl-5,7-bis(trifluoromethyl)pyrazolo[1,5-a]pyrimidin-3-yl]-phenol
SMILES: OC(C=C1)=CC=C1C(C(C2=CC=CC=C2)=N3)=C4N3C(C(F)(F)F)=CC(C(F)(F)F)=N4
Formula: C20H11F6N3O
M.Wt: 423.3
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: PHTPP is a selective ERβ antagonist.
In Vitro: PHTPP is a selective ERβ antagonist. PHTPP reduces FSH-mediated cAMP production by 80% (p<0.01) while it has no effect on basal cAMP[1]. PHTPP (10-6 M) inhibits E2-stimulated ERβ activity, but does not suppress E2-stimulated ERα activity. A high dose of PHTPP (10-6 M) slightly increases class 1 Igf1 mRNA expression, and facilitates the DPN-induced increase in class 1 Igf1 mRNA expression[2].
COA
MSDS
Cat. No. Product name Field of application
DC46877 Y134 Y134 is a selective and orally active oestrogen receptor (ER) modulator (SERM), exhibits potent antagonist activity at ERα and ERβ. Y134 shows 121.1-fold selectivity for ERα (Ki=0.09 nM) over ERβ (Ki=11.31 nM).
DC42456 Camizestrant ( AZD-9833) Camizestrant (AZD-9833) is a potent and orally active estrogen receptor (ER) antagonist. Camizestrant is used for the study of ER+ HER2-advanced breast cancer.
DC26134 PROTAC ERRα ligand 2 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)[1].
DC7735 XCT790 XCT-790 is a potent, selective and inverse agonist of estrogen-related receptor alpha(ERRα); induces cell death in chemotherapeutic resistant cancer cells.
DC10077 WAY-200070 WAY-200070 is a potent, selective estrogen receptor-beta (ER-β) agonist (IC50 2.3 nM vs 155 nM for ER-α) with anxiolytic-like and antidepressant-like effects.
DC10846 PHTPP PHTPP is a pyrazolo[1,5-α]pyrimidine-based ligand that acts as a full antagonist of estrogen ERβ receptors with 36-fold selectivity over ERα.
DC10755 LSZ-102 LSZ102 is a potent, orally bioavailable Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen Receptor Positive Breast Cancer.
DCAPI1501 Lasofoxifene tartrate Lasofoxifene Tartrate is a non-steroidal selective estrogen receptor modulator (SERM).
DC8265 Endoxifen Endoxifen is a Estrogen receptor α (ERα) ligand; potent antiestrogen,an active metabolite of the cancer drug tamoxifen.
DC9959 Endoxifen (E-isomer) Endoxifen (E-isomer hydrochloride) is a tamoxifen metabolite and potent Selective Estrogen Response Modifier (SERM).
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