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MGL-3196 is a selective thyroid hormone receptor β agonist with EC50s of 0.21 and 3.74 µM for TRβ and TRα respectively.
Afimoxifene is the active metabolite of tamoxifen and a selective estrogen receptor (ER) modulator that is widely used in the therapeutic and chemopreventive treatment of breast cancer. Afimoxifene is a potent activator of ER and has been shown to have a higher affinity for estrogen receptors compared to tamoxifen. It has significant dose and time-dependent direct effects to alter the contractile function of isolated adult rat cardiac myocytes. This product has no specified isomer.
Diethylstilbestrol is a synthetic nonsteroidal estrogen that produces all the pharmacological and therapeutic effects of natural estradiol. It is mainly used for functional hemorrhage caused by estrogen hypoxia and hormonal imbalance, amenorrhea.
Genistin is a isoflavone which has a role in blocking cell cycle and inducing apoptosis. It is also a modulator of estrogen receptor. Genistin can be isolated from the seeds of glycine max (L.) merr. and used as negative control of genistein.
Endoxifen Z-isomer HCl is the most important Tamoxifen metabolite responsible for eliciting the anti-estrogenic effects of this drug in breast cancer cells expressing estrogen receptor-alpha (ERα). Endoxifen Z-isomer HCl inhibits hERG tail currents at 50 mV in a concentration-dependent manner with IC50 values of 1.6 μM.
Selective, high affinity silent antagonist at ERα receptors. Displays > 200-fold selectivity for ERα over ERβ. Ki values are 2.7 and 1800 nM at ERα and ERβ receptors respectively.
Liquiritigenin is an estrogenic compound which fuctions as a selective agonist of the estrogen receptor ERβ and an partial agonist of ERα. It also has choleretic effect. Liquiritigenin is a flavanone extracted from glycyrrhiza uralensis with antitumour action.
Kaempferol acts as an inverse agonist that directly binds ERRα and ERRγ. It is a natural flavonol with antitumor activity.
Licochalcone A, an estrogenic flavanoid, can be an inhibitor of p-glycoprotein and has anti-inflammatory actions.
PCO371 is an orally active full agonist of parathyroid hormone receptor 1 (PTHR1), shows no effect on PTH type 2 receptor.
Tags: ERR | 内分泌学/激素 | Endocrinology/Hormones | ERR 相关产品
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