1. Signaling Pathways
  2. Metabolic Enzyme/Protease
  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 (19):

目录号 产品名 作用方式 纯度
  • HY-B0561
    Spironolactone Antagonist 99.05%
    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)。
  • HY-16276
    Osilodrostat Inhibitor 99.90%
    Osilodrostat (LCI699) 是人11β-羟化酶和醛固酮合成酶的有效抑制剂,IC50分别值为2.5 和0.7nM。
  • HY-100471
    Esaxerenone Antagonist 99.88%
    Esaxerenone (CS-3150) 是一种高度有效且有选择性的非类固醇盐皮质激素受体拮抗剂。
  • HY-109017
    Vamorolone Antagonist 99.12%
    Vamorolone (VBP15) 是首创的,具有口服活性的解离性类固醇 (dissociative steroidal) 抗炎药和膜稳定剂。Vamorolone 改善肌营养不良,无副作用。Vamorolone 抑制 (NF-κB) 抑制作用,并降低了激素的影响。
  • HY-B0251
    Eplerenone Antagonist 99.68%
    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。
  • 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)。
  • HY-132809
    Baxdrostat Inhibitor
    Baxdrostat 是一种醛固酮合成酶抑制剂。
  • 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)。
  • HY-B1472
    Deoxycorticosterone acetate Agonist ≥98.0%
    Deoxycorticosterone 醋酸盐是一种肾上腺皮质素, 作为前体醛固酮。
  • HY-111372
    Finerenone Antagonist 99.95%
    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。
  • HY-B1203A
    Fludrocortisone acetate Agonist 99.45%
    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。
  • HY-B1438
    Canrenone Antagonist 99.54%
    Canrenone (Aldadiene) 是广泛用作利尿剂的醛固酮 (aldosterone) 拮抗剂。
  • HY-109002
    Apararenone Antagonist 98.98%
    Apararenone (MT-3995) 是新型非甾体类盐皮质激素受体 (mineralocorticoid receptor) 拮抗剂,正在开发用于研究糖尿病性肾病和非酒精性脂肪性肝炎。
  • HY-120274
    AZD9977 Modulator 99.85%
    AZD9977 是一种有效的,选择性的,具有口服活性的盐皮质激素受体 (MR) 调节剂。AZD9977 用于心力衰竭和慢性肾病的研究。
  • HY-113151
    18-Oxocortisol Antagonist
    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。
  • HY-B1203
    Fludrocortisone Agonist
    Fludrocortisone是一种合成的盐皮质激素,具有抗炎功能。
  • HY-12738
    PF-3882845 Antagonist
    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。
  • HY-B1582A
    Canrenoate potassium Antagonist 99.37%
    Canrenoate potassium 是一种释放 canrenone 的前药,也是一种有效的竞争性盐皮质激素受体 (mineralocorticoid receptor) 拮抗剂。Canrenoate potassium 作为一种利尿剂,用于高血压的研究。
  • HY-U00200
    Dicirenone 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。
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