1. Signaling Pathways
  2. Metabolic Enzyme/Protease
    Vitamin D Related/Nuclear Receptor
  3. Mineralocorticoid Receptor

Mineralocorticoid Receptor (盐皮质激素受体)

Mineralocorticoid receptor (MR) is an intracellular steroid hormone receptor, and a member of the nuclear receptor superfamily, that mediates the physiological action of two important adrenal steroids, aldosterone and cortisol. Mineralocorticoid receptor is closely related to the glucocorticoid receptor (GR), and it can indifferently bind mineralocorticoid and glucocorticoid hormones. Activation of the mineralocorticoid receptor in the distal nephron by its ligand, aldosterone, plays an important role in sodium reabsorption and blood pressure regulation. Besides the regulation of sodium balance and the control of blood pressure, aldosterone-human mineralocorticoid receptor tandem also exerts important regulatory functions on the cardiovascular and central nervous systems.

Mineralocorticoid receptor participates in the regulation of hydroelectrolytic homeostasis in sodium-transporting tight epithelia such as distal nephron, colon, lung, and salivary and sweat glands. In such epithelial target cells, the mineralocorticoid specificity of aldosterone action is given by the enzyme 11β-hydroxysteroid dehydrogenase 2 (11-HSD2), which converts active glucocorticoids into inactive metabolites. Mineralocorticoid receptor is also expressed in nonepithelial tissues such as the heart, some areas of the brain, large blood vessels, and mononuclear leukocytes. The ligand-activated mineralocorticoid receptor is translocated in the nucleus and acts as a transcription factor after its interaction with the consensus glucocorticoid response element (GRE) sequences. Mineralocorticoid receptor could activate or inhibit transcription of target genes whose identification is under intense investigation.

Mineralocorticoid Receptor 相关产品 (47):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-B1438S
    Canrenone-d6

    坎利酮-d6

    Antagonist
    Canrenone-d6 是 Canrenone 的氘代物。Canrenone (Aldadiene) 是广泛用作利尿剂的醛固酮 (aldosterone) 拮抗剂。
    Canrenone-d<sub>6</sub>
  • HY-B0251S
    Eplerenone-d3

    依普利酮 d3

    Antagonist
    Eplerenone-d3 是 Eplerenone 的氘代物。Eplerenone (Epoxymexrenone) 是一种选择性,竞争性和具有口服活性的醛固酮 (aldosterone) 拮抗剂,IC50 为 138 nM。Eplerenone 对孕酮,雄激素,雌激素和糖皮质激素受体的亲和力低。Eplerenone 可用于高血压和心肌梗死后的心力衰竭的研究。
    Eplerenone-d<sub>3</sub>
  • HY-163689
    Vicadrostat
    Vicadrostat 是一种醛固酮合成酶 (aldosterone synthase) 抑制剂 (IC50=48 nM)。Vicadrostat 可用于肾脏疾病和心血管疾病的研究。
    Vicadrostat
  • HY-163751
    STING-IN-9 Inhibitor
    STING-IN-9 (compound 2) 是人 CYP11B2 的有效抑制剂。体外实验中,STING-IN-9 的选择性比人 CYP11B1 高 80 倍以上。
    STING-IN-9
  • HY-111372S
    Finerenone-d3
    Finerenone-d3 是氘标记的 Finerenone (HY-111372)。Finerenone (BAY 94-8862) 是第三代选择性、具有口服活性的、非甾体类盐皮质激素受体 (MR) 拮抗剂 (IC50=18 nM)。与糖皮质激素受体 (GR)、雄激素受体 (AR) 和孕酮受体 (AR) 相比,Finerenone 表现出良好的选择性 (>500-fold)。Finerenone 在心肾疾病研究中具有潜在的应用前景,如 2 型糖尿病和慢性肾脏疾病。
    Finerenone-d<sub>3</sub>
  • HY-136969
    RU 752 Antagonist
    RU 752 是一种有效的盐皮质激素受体 (I 型或 MR) 拮抗剂。
    RU 752
  • HY-U00200
    Dicirenone

    地西利酮

    Antagonist
    Dicirenone (SC26304) 抑制醛固酮对尿 K+:Na+ 比例的调节作用,也抑制 [3H] 醛固酮与肾细胞质和核受体结合作用。
    Dicirenone