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Chemical Structure| 805239-56-9 Chemical Structure| 805239-56-9

Structure of PHTPP
CAS No.: 805239-56-9

Chemical Structure| 805239-56-9

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PHTPP has selective antagonism of estrogen ERβ receptor .

4.5 *For Research Use Only !

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Product Details of PHTPP

CAS No. :805239-56-9
Formula : C20H11F6N3O
M.W : 423.31
SMILES Code : OC1=CC=C(C2=C3N=C(C(F)(F)F)C=C(C(F)(F)F)N3N=C2C4=CC=CC=C4)C=C1
MDL No. :MFCD09971112
InChI Key :AEZPAUSGTAHLOQ-UHFFFAOYSA-N
Pubchem ID :11201035

Safety of PHTPP

GHS Pictogram:
Signal Word:Danger
Hazard Statements:H301
Precautionary Statements:P301+P310
Class:6.1
UN#:2811
Packing Group:

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Fibroblast-like synoviocytes (FLSs) 5 nM 24 hours PHTPP partially reversed the upregulation of GPX4, LPAR3, and ESR2 in FLSs induced by LXA4 PMC11126537
Patient-derived BSCs 100 nM 12 days PHTPP significantly reduces mammosphere formation PMC5441302
MCF7 cells 100 nM 24 hours PHTPP inhibits ERβ-mediated glycolytic metabolism PMC5441302
Human uterine artery endothelial cells (hUAECs) 1 μM 24 hours To investigate the effect of PHTPP (ERβ antagonist) on estradiol-stimulated AT2R expression. Results showed that PHTPP completely attenuated estradiol-induced AT2R mRNA and protein expression. PMC6739159
Pregnant ovine uterine artery endothelial cells (P-UAECs) 1 μmol/L 1 hour PHTPP did not inhibit E2β-induced PGI2 production in P-UAECs, indicating that E2β-induced PGI2 production is primarily mediated via ER-α and independent of ER-β PMC3924857
Rat thoracic aorta vascular smooth muscle cells (VSMCs) 5 μmol/L PHTPP, as a specific ERβ antagonist, was used to block the inhibitory effect of farrerol on VSMC proliferation, showing that PHTPP significantly attenuated the inhibitory effect of farrerol PMC4001983
Neonatal rat cardiomyocytes 100 nM PHTPP prevented the inhibition of BMP4-induced BMP4 protein expression by estrogen PMC4667872

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
SD rats MIA-induced KOA model Intraperitoneal injection 100 μg/kg Injected before each exercise session for 4 weeks PHTPP partially reversed the improvement in pain behavior and joint pathology in KOA rats induced by treadmill exercise PMC11126537
NOD/SCID mice MCF7 xenograft model Daily injections 4 mg/kg Daily for five weeks PHTPP significantly reduces tumor volume PMC5441302
C57BL/6J mice Cyclophosphamide-induced DOR model Intraperitoneal injection 2 mg/kg or 4 mg/kg Every other day for 14 days To evaluate the therapeutic effect of PHTPP on DOR model mice. Results showed that PHTPP treatment restored normal sex hormone secretion, estrus cycle duration, follicle development, oocyte quality, and litter size. PMC11745447

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.36mL

0.47mL

0.24mL

11.81mL

2.36mL

1.18mL

23.62mL

4.72mL

2.36mL

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