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.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO: 13 mg/mL (warmed)|
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.
|Related Estrogen Receptor Products|
|Endoxifen E-isomer hydrochloride
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Relugolix, also known as TAK-385, is a luteinizing hormone-releasing hormone (LH-RH) receptor antagonist with an IC50 of 0.12 nM.
Elagolix Soidum is a potent, selective, orally active, non-peptide antagonist of the gonadotropin-releasing hormone receptor (GnRHR) with Kd value of 54 pM.
GDC-0810 (Brilanestrant, ARN-81) is an orally bioavailable selective estrogen receptor degrader (SERD) with IC50 of 0.7 nM.
G15 is a high affinity and selective G-protein-coupled estrogen receptor (GPER/GPR30) antagonist with a Ki of 20 nM.
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