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PHTPP

Catalog No. T4388 CAS 805239-56-9

PHTPP is a selective ERβ antagonist.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

PHTPP, CAS 805239-56-9

Pack Size	Availability	Price/USD
2 mg	In stock	$ 38.00
5 mg	In stock	$ 61.00
10 mg	In stock	$ 93.00
25 mg	In stock	$ 182.00
50 mg	In stock	$ 297.00
100 mg	In stock	$ 459.00
500 mg	In stock	$ 987.00
1 mL * 10 mM (in DMSO)	In stock	$ 66.00

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Purity: 99.72%

Purity: 99.37%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	PHTPP is a selective ERβ antagonist.
In vitro	PHTPP acts as a selective antagonist for estrogen receptor beta (ERβ), significantly decreasing follicle-stimulating hormone (FSH)-mediated cyclic AMP (cAMP) production by 80% (p<0.01), without impacting basal cAMP levels. At a concentration of 10^-6 M, PHTPP inhibits estradiol (E2)-stimulated ERβ activity but does not affect E2-induced ERα activity. Furthermore, a high concentration of PHTPP (10^-6 M) marginally enhances class 1 Igf1 mRNA expression and promotes the DPN-induced increase in class 1 Igf1 mRNA expression.
Cell Research	Cells are plated at a density of 3 to 4×10^5 in 1 mL of medium per well in a 24-well plate for cell viability and cAMP analysis. Cells are cultured in Dulbecco's Modified Eagle Medium with PHTPP (1 μM), or ethanol (0.1%) as the vehicle. The incubator is set to an atmosphere of 5% CO2 in air at 37°C, and cultures are allowed to acclimate for at least 24 h. The culture medium is then aspirated and replaced with serum-free DMEM/F12 containing 0.1 μM androstenedione. The cells are collected for intracellular cAMP and to test cell viability. They are for reference only.

Molecular Weight	423.31
Formula	C20H11F6N3O
CAS No.	805239-56-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 14 mg/mL(33 mM)

References and Literature

1. Compton DR, etal. Pyrazolo[1,5-a]pyrimidines: estrogen receptor ligands possessing estrogen receptor beta antagonist activity. J Med Chem. 2004 Nov 18;47(24):5872-93. 2. Wang K, Chen Y, Gao S, et al. Norlichexanthone purified from plant endophyte prevents postmenopausal osteoporosis by targeting ERα to inhibit RANKL signaling[J]. Acta Pharmaceutica Sinica B. 2020

Citations

1. Wang K, Chen Y, Gao S, et al. Norlichexanthone purified from plant endophyte prevents postmenopausal osteoporosis by targeting ERα to inhibit RANKL signaling[J].. Acta Pharmaceutica Sinica B. 2021, 11(2): 442-455 2. Wang K, Chen Y, Gao S, et al Norlichexanthone purified from plant endophyte prevents postmenopausal osteoporosis by targeting ERα to inhibit RANKL signaling. Acta Pharmaceutica Sinica B. 2020 3. Cui S, Suo N, Yang Y, et al.The aminosteroid U73122 promotes oligodendrocytes generation and myelin formation.Acta Pharmacologica Sinica.2023: 1-12.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library ReFRAME Related Library Anti-Ovarian Cancer Compound Library Anti-Cancer Compound Library Bioactive Compounds Library Max Fluorochemical Library Human Metabolite Library Target-Focused Phenotypic Screening Library Endocrinology-Hormone Compound Library NO PAINS Compound Library

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Keywords

PHTPP 805239-56-9 Endocrinology/Hormones Estrogen/progestogen Receptor Estrogen Receptor/ERR Inhibitor inhibit inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.