Abcam, ab141251, Eplerenone, Selective mineralocorticoid antagonist

Size: 10mg / 50mg
MW 414.5 Da, Purity >99%. Selective mineralocorticoid (aldosterone) antagonist (IC 50 = 81 nM). Significantly greater selectivity than spironolactone at androgen, progesterone and glucocorticoid receptors. Antihypertensive, orally active in vivo .
Key facts
CAS number:107724-20-9,
Purity:>99%,
Form:SolidSee storage information,
Molecular weight:414.5 Da,
Molecular formula:C24H30O6,
PubChem:443872,
Nature:Synthetic,
Solubility:Soluble in DMSO to 10 mM,
Biochemical name:Eplerenone,
Biological description:Selective mineralocorticoid (aldosterone) antagonist (IC50 = 81 nM). Significantly greater selectivity than spironolactone at androgen, progesterone and glucocorticoid receptors. Antihypertensive, orally active in vivo.,
Canonical smiles:CC12CCC(=O)C=C1CC(C3C24C(O4)CC5(C3CCC56CCC(=O)O6)C)C(=O)OC,
Isomeric smiles:C[C@]12CCC(=O)C=C1C[C@H]([C@@H]3[C@]24[C@H](O4)C[C@]5([C@H]3CC[C@@]56CCC(=O)O6)C)C(=O)OC,
InChi:InChI=1S/C24H30O6/c1-21-7-4-14(25)10-13(21)11-15(20(27)28-3)19-16-5-8-23(9-6-18(26)30-23)22(16,2)12-17-24(19,21)29-17/h10,15-17,19H,4-9,11-12H2,1-3H3/t15-,16+,17-,19+,21+,22+,23-,24-/m1/s1,
InChiKey:JUKPWJGBANNWMW-VWBFHTRKSA-N,
IUPAC Name:methyl (1R,2S,9R,10R,11S,14R,15S,17R)-2,15-dimethyl-5,5'-dioxospiro[18-oxapentacyclo[8.8.0.01,17.02,7.011,15]octadec-6-ene-14,2'-oxolane]-9-carboxylate

Properties and Storage Information:
Shipped at conditions-Ambient - Can Ship with Ice, Appropriate short-term storage conditions-+4°C, Appropriate long-term storage conditions-+4°C, Storage information-Store under desiccating conditions, The product can be stored for up to 12 months

Supplementary Information:
This supplementary information is collated from multiple sources and compiled automatically.
Glucocorticoid Receptor (GR) Progesterone Receptor (PR) Mineralocorticoid Receptor (MR) and Androgen Receptor (AR) belong to the nuclear receptor superfamily. Each receptor functions as a ligand-activated transcription factor that regulates gene expression. These receptors typically share a similar mass ranging from 90 to 100 kDa and are widely expressed in various tissues. GR is widely found in almost every cell PR is mainly present in female reproductive tissues MR predominantly locates in kidney and heart while AR primarily exists in androgen-responsive tissues such as prostate.
Biological function summary
These receptors play critical roles in regulating numerous physiological processes. They are involved in complex interactions with cofactors and DNA to influence transcription. GR regulates stress responses and immune function. PR plays a role in the menstrual cycle and pregnancy while MR maintains electrolyte balance. AR influences male sexual development and metabolic processes. These receptors form part of larger complexes that modify chromatin and facilitate gene transcription in response to specific hormones.
Pathways
These receptors integrate into vital hormonal signaling pathways. The GR is important in the hypothalamic-pituitary-adrenal (HPA) axis interacting with HSP90 and other chaperone proteins for proper folding and activity. The PR functions in reproductive hormone signaling interacting with pathways that include the Estrogen Receptor (ER). These pathways are intricately connected ensuring fine regulation of hormone actions and cross-talk between different hormonal signals.
Dysregulation of these receptors links to various conditions. GR malfunction ties to Cushing's syndrome and glucocorticoid resistance involving impaired regulation with proteins like MAPKs. PR imbalances relate to reproductive disorders such as endometriosis and infertility. The MR is closely monitored in relation to hypertension and heart failure often targeted by mineralocorticoid antagonists like eplerenone which directly affects electrolyte homeostasis. AR alterations have associations with prostate cancer with clinical impacts on proteins such as PSA in tumor development and progression.