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 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 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|
GDC-0810 (Brilanestrant, ARN-81) is an orally bioavailable selective estrogen receptor degrader (SERD) with IC50 of 0.7 nM.
GSK 4716 is a selective agonist with estrogen-related receptors ERRβ and ERRγ.
RaloxifeneHcl(LY156758 Hcl) is a second generation selective estrogen receptor antagonist.
Progesterone is an endogenous steroid hormone involved in the menstrual cycle, pregnancy, and embryogenesis of humans and other species. A potent agonist of the nuclear progesterone receptor (nPR) with Kd of 1 nM; An agonist of the membrane progesterone receptors(mPRs); An antagonist of the σ1 receptor.
Megestrol acetate is a synthetic progestogen, used to treat breast cancer and loss of appetite.
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