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 (42):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-113151
    18-Oxocortisol Antagonist ≥98.0%
    18-Oxocortisol 是由醛固酮合酶 (CYP11B2) 产生的皮质醇衍生物。18-Oxocortisol 是天然存在的盐皮质激素 (mineralocorticoid) 激动剂。18-Oxocortisol 是肾上腺静脉采样中的生物标志物。
    18-Oxocortisol
  • HY-111372A
    (Rac)-Finerenone Antagonist 99.66%
    (Rac)-Finerenone ((Rac)-BAY 94-8862) 是 Finerenone 的外消旋体。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)。
    (Rac)-Finerenone
  • HY-16276A
    Osilodrostat phosphate Inhibitor 99.35%
    Osilodrostat (LCI699) phosphate 是一种口服有效的 11β-羟化酶 (CYP11B1) 抑制剂,其 IC50 值为 35 nM。Osilodrostat phosphate 是一种口服有效的醛固酮合成酶 (CYP11B2) 抑制剂,抑制人醛固酮合成酶和大鼠醛固酮合成酶的 IC50 分别为 0.7 nM 和 160 nM。Osilodrostat phosphate 抑制醛固酮和皮质酮的合成。Osilodrostat phosphate 具有降低血压的能力。Osilodrostat phosphate 可用于库欣综合征 (CS) 的研究。
    Osilodrostat phosphate
  • HY-132827
    Ocedurenone Antagonist
    Ocedurenone 是一种 皮质类固醇受体 拮抗剂。Ocedurenone 可用于肾脏疾病的研究 (WO2018054357,化合物 I)。
    Ocedurenone
  • HY-12738
    PF-3882845 Antagonist 99.90%
    PF-3882845 是一种高亲和力的,口服有效的选择性盐皮质激素受体 (MR; 结合 IC50=2.7 nM) 拮抗剂,有潜力用于高血压和肾病的研究。PF-3882845 还与孕激素受体 (PR) 结合,结合 IC50 为 310 nM。
    PF-3882845
  • HY-B0561S
    Spironolactone-d7

    螺内酯 d7

    Antagonist 99.96%
    Spironolactone-d7 是 Spironolactone 的氘代物。Spironolactone (SC9420) 是一种具有口服活性醛固酮盐皮质激素受体 (aldosterone mineralocorticoid receptor) 拮抗剂,IC50 值为 24 nM。Spironolactone 也是雄激素受体 (androgen receptor) 拮抗剂,IC50
    Spironolactone-d<sub>7</sub>
  • HY-107631
    Oxprenoate potassium Antagonist ≥98.0%
    Oxprenoate potassium 是一种有效的 mineralocorticoid (MR) 拮抗剂。Oxprenoate potassium 增强 DEX (地塞米松) 诱导的细胞凋亡 (apoptosis
    Oxprenoate potassium
  • HY-B0561S1
    Spironolactone-d3

    螺内酯 d3

    Antagonist 99.82%
    Spironolactone-d3 是 Spironolactone 的氘代物。Spironolactone (SC9420) 是一种具有口服活性醛固酮盐皮质激素受体 (aldosterone mineralocorticoid receptor) 拮抗剂,IC50 值为 24 nM。Spironolactone 也是雄激素受体 (androgen receptor) 拮抗剂,IC50
    Spironolactone-d<sub>3</sub>
  • HY-B1203
    Fludrocortisone

    氟氢可的松

    Agonist ≥98.0%
    Fludrocortisone是一种合成的盐皮质激素,具有抗炎功能。
    Fludrocortisone
  • HY-B1203S
    Fludrocortisone-d5

    氟氢可的松-d5

    Agonist
    Fludrocortisone-d5 是 Fludrocortisone 的氘代物。Fludrocortisone是一种合成的盐皮质激素,具有抗炎功能。
    Fludrocortisone-d<sub>5</sub>
  • HY-B1438S1
    Canrenone-d4

    坎利酮-d4

    Antagonist
    Canrenone-d4 是 Canrenone 氘代物。Canrenone (Aldadiene) 是广泛用作利尿剂的醛固酮 (aldosterone) 拮抗剂。
    Canrenone-d<sub>4</sub>
  • HY-132809A
    (S)-Baxdrostat Inhibitor 98.84%
    (S)-Baxdrostat 是 Baxdrostat 的 S-对映异构体。Baxdrostat 是一种醛固酮合酶 (aldosterone synthase) 抑制剂。
    (S)-Baxdrostat
  • HY-B1203AR
    Fludrocortisone acetate (Standard)

    醋酸氟氢可的松(标准品)

    Agonist 98.77%
    Fludrocortisone acetate (Standard) 是 Fludrocortisone acetate 的分析标准品。本产品用于研究及分析应用。Fludrocortisone acetate (9α-Fludrocortisone acetate) 是一种合成的盐皮质激素, 有潜力用于阿狄森氏病的研究,可减少尿液中钠丢失量, 也用于增加血压。
    Fludrocortisone acetate (Standard)
  • HY-B1203AS
    Fludrocortisone acetate-d5

    醋酸氟氢可的松-d5

    Agonist
    Fludrocortisone acetate-d5 是 Fludrocortisone acetate 氘代物。Fludrocortisone acetate (9α-Fludrocortisone acetate) 是一种合成的盐皮质激素, 有潜力用于阿狄森氏病的研究,可减少尿液中钠丢失量, 也用于增加血压。
    Fludrocortisone acetate-d<sub>5</sub>
  • HY-B1472R
    Deoxycorticosterone acetate (Standard)

    醋酸去氧皮质酮(标准品)

    Agonist 99.32%
    Deoxycorticosterone acetate (Standard) 是 Deoxycorticosterone acetate 的分析标准品。本产品用于研究及分析应用。Deoxycorticosterone acetate (DOCA) 是一种肾上腺皮质激素,是醛固酮的前体。Deoxycorticosterone acetate 是一种矿化皮质激素受体激动剂。Deoxycorticosterone acetate 可导致严重的肾脏损伤,包括炎症、纤维化、肾小球损伤和蛋白尿。
    Deoxycorticosterone acetate (Standard)
  • HY-B1203S1
    Fludrocortisone-d2

    氟氢可的松-d2

    Agonist
    Fludrocortisone-d2 是 Fludrocortisone 氘代物。Fludrocortisone是一种合成的盐皮质激素,具有抗炎功能。
    Fludrocortisone-d<sub>2</sub>
  • HY-B0561S2
    Spironolactone-d3-1

    螺内酯-d3

    Antagonist
    Spironolactone-d3-1 是 Spironolactone 氘代物。Spironolactone (SC9420) 是一种具有口服活性醛固酮盐皮质激素受体 (aldosterone mineralocorticoid receptor) 拮抗剂,IC50 值为 24 nM。Spironolactone 也是雄激素受体 (androgen receptor) 拮抗剂,IC50 为 77 nM。Spironolactone 促进足细胞自噬 (autophagy)。
    Spironolactone-d<sub>3</sub>-1
  • 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-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>