Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T2339 |
Apalutamide
ARN-509 |
Androgen Receptor; GABA Receptor | Endocrinology/Hormones; Membrane transporter/Ion channel; Neuroscience |
Apalutamide (ARN-509) 是一种有效、竞争性的雄激素受体 (AR) 拮抗剂(IC50:16 nM)。 | |||
T12146 |
N-Desmethyl-Apalutamide
N-Desmethyl Apalutamide,N-去甲基阿帕鲁胺杂质 |
P450; Androgen Receptor | Endocrinology/Hormones; Metabolism |
N-Desmethyl-Apalutamide 是一种 Apalutamide 的活性代谢产物,主要由 CYP2C8 和 CYP3A4 介导形成。它是一种低活性的雄激素受体拮抗剂,其作用力是 Apalutamide 活性的三分之一。它是中等至强的CYP3A4和CYP2B6诱导剂,并具有优异的血浆蛋白结合浓度。 | |||
T38725 |
Apalutamide-COOH
|
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Apalutamide-COOH is a metabolite derived from Apalutamide, which acts as a highly potent and competitive antagonist of the androgen receptor (AR). It effectively binds to the AR with an IC50 value of 16 nM. |