Methylpiperidino pyrazole (MPP) is an agonist for estrogen receptor α and lacks any ligand functionality with estrogen receptor (ER)β. Methyl-piperidino-pyrazole promotes silibinin induced apoptosis in human breast cancer MCF-7 cells.
|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 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.
|Solubility||DMSO 5 mg/mL|
Analogs of methyl-piperidinopyrazole (MPP): antiestrogens with estrogen receptor alpha selective activity
Hai-Bing Zhou, et al. Bioorg Med Chem Lett. 2009 Jan 1;19(1):108-10. PMID: 19014882.
The effects of the selective estrogen receptor modulators, methyl-piperidino-pyrazole (MPP), and raloxifene in normal and cancerous endometrial cell lines and in the murine uterus
Angela M Davis, et al. Mol Reprod Dev. 2006 Aug;73(8):1034-44. PMID: 16688783.
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|Endoxifen E-isomer hydrochloride
Endoxifen E-isomer hydrochloride is a tamoxifen metabolite and potent Selective Estrogen Response Modifier (SERM).
Relugolix, also known as TAK-385, is a luteinizing hormone-releasing hormone (LH-RH) receptor antagonist with an IC50 of 0.12 nM.
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