Finerenone

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Cat Number

API1050477310

CAS Number

1050477-31-0

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Product Detail Description Scientific Support Customer Q&A

CAS Number

1050477-31-0

Storage

Store at room temperature

Synonyms

BAY 94-8862

Molecular Formula

C21H22N4O3

Molecular Weight

378.424

Smiles

CCOC1=NC=C(C2=C1[C@@H](C(=C(N2)C)C(=O)N)C3=C(C=C(C=C3)C#N)OC)C

Standard

In-house
Facility GMP

Qualification

DMF/CDE

General Description

Finerenone is a selective the drug mineralocorticoid receptor antagonist, developed for use in the treatment of chronic kidney disease (CKD) and type 2 diabetes. It was recently discovered to also have an add on role in the management of resistant hypertension.

Mechanism of Action

Finerenone antagonizes the effects of mineralocorticoids (such as aldosterone and cortisol) when MR is overactivated, thereby may ameliorate cardiac and kidney inflammation and fibrosis. Aldosterone is secreted from the activation of the RAAS pathway; this pathway is involved in the regulation of blood pressure and sodium and fluid retention.

Application

Finerenone, a third-generation non-steroidal mineralocorticoid receptor antagonist, offers multiple benefits via anti-fibrotic, anti-inflammatory, and oxidative stress-reducing effects. It shows efficacy in treating type 2 diabetes mellitus-related chronic kidney disease (T2DM-CKD), reducing renal and cardiovascular event risks per trials like FIDELIO-DKD and FIGARO-DKD. Preclinically, it improves vascular function, metabolic health, and diabetic retinopathy. While approved for T2DM-CKD, ongoing trials explore its use in non-diabetic CKD, type 1 diabetes-related CKD, and primary aldosteronism. It has a favorable safety profile vs. traditional MRAs but requires potassium monitoring; potential cancer risks need further validation. Authoritative guidelines recommend it, highlighting its promise in cardio-renal-metabolic disease management.

The MR is expressed in a wide variety of cell types, including endothelial cells, vascular smooth muscle cells, fibroblasts, macrophages, mesangial cells, and podocytes. Hyperactivity of the MR causes upregulation of inflammatory and fibrotic target genes, which can lead to organ damage. Inhibition of the MR prevents cellular injury by suppressing oxidative stress and inflammatory pathways. Finerenone selectively binds to the MR and blocks the MR as a large, passive antagonist. Binding of finerenone to the MR alters the conformation of the receptor in a manner distinct from the changes induced by steroid hormones or steroidal MR antagonists. This interaction prevents the recruitment of cell-specific cofactors to the MR, which in turn causes alterations in the expression of downstream target genes, including those that are proinflammatory and profibrotic.

Fig. 1 Proposed mode of action and pharmacology of finerenone. (Lerma EV, Wilson D J. 2022)

References

Lerma EV, Wilson D J. Finerenone: a mineralocorticoid receptor antagonist for the treatment of chronic kidney disease associated with type 2 diabetes. Expert Review of Clinical Pharmacology. 2022, 15(5): 501-513.

Do you provide a certificate of analysis for each Finerenone batch?

Yes, every shipment of Finerenone includes a detailed certificate of analysis (COA).

Is Finerenone sensitive to moisture during long-term storage?

Yes, Finerenone should be kept in airtight, moisture-proof packaging to maintain its physical and chemical stability.

How can I track my Finerenone order?

Use the tracking number provided to follow your Finerenone order.

Can I cancel my Finerenone order after placing it?

Yes, cancellations must be made before shipping Finerenone.