LY500307 potently binds both ERα and ERβ with Ki value of 2.68 nM and 0.19 nM. LY500307 displays potent inhibition toward ERβ with EC50 of 0.66 nM and shows full agonist function in estrogen receptor beta (ERbeta) in vitro assays (>90% relative efficacy).
|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 50 mg/mL
Ethanol 50 mg/mL
Benzopyrans are selective estrogen receptor beta agonists with novel activity in models of benign prostatic hyperplasia.
Norman BH, et al. J Med Chem. 2006 Oct 19;49(21):6155-7. PMID: 17034120.
|Related Estrogen Receptor Products|
27-Hydroxycholesterol is a selective estrogen receptor modulator, and it is also an agonist of the liver X receptor.
SAR439859 (Amcenestrant) is an orally active, nonsteroidal and selective degrader of estrogen receptor, it is also a potent antagonist of ER with EC50 of 0.2 nM for ERα degradation.
4-Hydroxytamoxifen is a selective estrogen receptor modulator.
Methylpiperidino pyrazole (MPP) is an agonist for estrogen receptor α and lacks any ligand functionality with estrogen receptor (ER)β.
|Endoxifen E-isomer hydrochloride
Endoxifen E-isomer hydrochloride is a tamoxifen metabolite and potent Selective Estrogen Response Modifier (SERM).
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