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PHTPP

Cat. No. M8508
PHTPP Structure
Size Price Availability Quantity
10mM*1mL USD 65.7  USD73 In stock
5mg USD 63  USD70 In stock
10mg USD 108  USD120 In stock
25mg USD 234  USD260 In stock
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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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 423.31
Formula C20H11F6N3O
CAS Number 805239-56-9
Purity 97.49%
Solubility DMSO 13 mg/mL (warmed)
Storage at -20°C
References

IGF-1 gene expression is differentially regulated by estrogen receptors α and β in mouse endometrial stromal cells and ovarian granulosa cells
Yuki Ogo, et al. J Reprod Dev. 2014;60(3):216-23. PMID: 24670778.

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  Catalog
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Keywords: PHTPP supplier, Estrogen Receptor, inhibitors

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