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PHTPP

Cat. No. M8508
PHTPP Structure
Size Price Availability Quantity
10mM*1mL in DMSO USD 65  USD65 In stock
5mg USD 60  USD60 In stock
10mg USD 100  USD100 In stock
25mg USD 225  USD225 In stock
50mg USD 410  USD410 In stock
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Quality Control & Documentation
Biological Activity

PHTPP is a selective estrogen receptor β (ERβ) full antagonist with 36-fold selectivity for ERβ over ERα. PHTPP has been used to distinguish the various activites of the two estrogen receptors. Estrogen can have opposite effects in some tumors expressing ERα compared to Erβ, with Erα enhancing and Erβ suppressing tumor cell growth. PHTPP, a selective ERβ antagonist, significantly enhanced cell growth in ovarian cancer cell lines SKOV3 and OV2008 that express both receptors.

Product Citations
Chemical Information
Molecular Weight 423.31
Formula C20H11F6N3O
CAS Number 805239-56-9
Solubility (25°C) DMSO 13 mg/mL (warmed)
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Jaekyoon Kim, et al. Psychoneuroendocrinology. Distinct effects of estrogen receptor antagonism on object recognition and spatial memory consolidation in ovariectomized mice

[2] Yuki Ogo, et al. J Reprod Dev. IGF-1 gene expression is differentially regulated by estrogen receptors α and β in mouse endometrial stromal cells and ovarian granulosa cells

[3] T Samuel Dillon, et al. Behav Neurosci. 17β-estradiol enhances memory duration in the main olfactory bulb in CD-1 mice

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Keywords: PHTPP supplier, Estrogen Receptor, inhibitors, activators


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