WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H319698
CAS#: 1050477-31-0
Description: Finerenone, also known as BAY94-8862, is a non-steroidal antimineralocorticoid that is in phase III clinical trials for the treatment of chronic heart failure as of October 2015. It has less relative affinity to other steroid hormone receptors than currently available antimineralocorticoids such as eplerenone and spironolactone, which should result in fewer adverse effects like gynaecomastia, impotence, and low sex drive.
Hodoodo Cat#: H319698
Name: Finerenone
CAS#: 1050477-31-0
Chemical Formula: C21H22N4O3
Exact Mass: 378.17
Molecular Weight: 378.432
Elemental Analysis: C, 66.65; H, 5.86; N, 14.81; O, 12.68
Synonym: BAY94-8862; BAY 94-8862; BAY-94-8862; BAY948862; BAY 948862; BAY-948862; Finerenone
IUPAC/Chemical Name: (4S)-4-(4-Cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide
InChi Key: BTBHLEZXCOBLCY-QGZVFWFLSA-N
InChi Code: InChI=1S/C21H22N4O3/c1-5-28-21-18-17(14-7-6-13(9-22)8-15(14)27-4)16(20(23)26)12(3)25-19(18)11(2)10-24-21/h6-8,10,17,25H,5H2,1-4H3,(H2,23,26)/t17-/m1/s1
SMILES Code: O=C(C1=C(C)NC2=C(C(OCC)=NC=C2C)[C@@H]1C3=CC=C(C#N)C=C3OC)N
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
| Biological target: | |
| In vitro activity: | |
| In vivo activity: |
The following data is based on the product molecular weight 378.43 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
1: Bakris GL, Nowack C. Finerenone for Albuminuria in Patients With Diabetic Nephropathy--Reply. JAMA. 2016 Jan 19;315(3):306. doi: 10.1001/jama.2015.16014. PubMed PMID: 26784785.
2: Feng Y, Zeng X, Fu P. Finerenone for Albuminuria in Patients With Diabetic Nephropathy. JAMA. 2016 Jan 19;315(3):305-6. doi: 10.1001/jama.2015.15996. PubMed PMID: 26784783.
3: Bramlage P, Swift SL, Thoenes M, Minguet J, Ferrero C, Schmieder RE. Non-steroidal mineralocorticoid receptor antagonism for the treatment of cardiovascular and renal disease. Eur J Heart Fail. 2016 Jan;18(1):28-37. doi: 10.1002/ejhf.444. Epub 2015 Dec 3. Review. PubMed PMID: 26634965.
4: Lentini S, Heinig R, Kimmeskamp-Kirschbaum N, Wensing G. Pharmacokinetics, safety and tolerability of the novel, selective mineralocorticoid receptor antagonist finerenone - results from first-in-man and relative bioavailability studies. Fundam Clin Pharmacol. 2015 Nov 25. doi: 10.1111/fcp.12170. [Epub ahead of print] PubMed PMID: 26604072.
5: Newgard CD, Lewis RJ. Missing Data: How to Best Account for What Is Not Known. JAMA. 2015 Sep 1;314(9):940-1. doi: 10.1001/jama.2015.10516. PubMed PMID: 26325562.
6: Bakris GL, Agarwal R, Chan JC, Cooper ME, Gansevoort RT, Haller H, Remuzzi G, Rossing P, Schmieder RE, Nowack C, Kolkhof P, Joseph A, Pieper A, Kimmeskamp-Kirschbaum N, Ruilope LM; Mineralocorticoid Receptor Antagonist Tolerability Study–Diabetic Nephropathy (ARTS-DN) Study Group. Effect of Finerenone on Albuminuria in Patients With Diabetic Nephropathy: A Randomized Clinical Trial. JAMA. 2015 Sep 1;314(9):884-94. doi: 10.1001/jama.2015.10081. PubMed PMID: 26325557.
7: Amazit L, Le Billan F, Kolkhof P, Lamribet K, Viengchareun S, Fay MR, Khan JA, Hillisch A, Lombès M, Rafestin-Oblin ME, Fagart J. Finerenone Impedes Aldosterone-dependent Nuclear Import of the Mineralocorticoid Receptor and Prevents Genomic Recruitment of Steroid Receptor Coactivator-1. J Biol Chem. 2015 Sep 4;290(36):21876-89. doi: 10.1074/jbc.M115.657957. Epub 2015 Jul 22. PubMed PMID: 26203193; PubMed Central PMCID: PMC4571943.
8: Liu LC, Schutte E, Gansevoort RT, van der Meer P, Voors AA. Finerenone : third-generation mineralocorticoid receptor antagonist for the treatment of heart failure and diabetic kidney disease. Expert Opin Investig Drugs. 2015;24(8):1123-35. doi: 10.1517/13543784.2015.1059819. Epub 2015 Jun 20. PubMed PMID: 26095025.
9: Kolkhof P, Nowack C, Eitner F. Nonsteroidal antagonists of the mineralocorticoid receptor. Curr Opin Nephrol Hypertens. 2015 Sep;24(5):417-24. doi: 10.1097/MNH.0000000000000147. PubMed PMID: 26083526.
10: Pitt B, Anker SD, Böhm M, Gheorghiade M, Køber L, Krum H, Maggioni AP, Ponikowski P, Voors AA, Zannad F, Nowack C, Kim SY, Pieper A, Kimmeskamp-Kirschbaum N, Filippatos G. Rationale and design of MinerAlocorticoid Receptor antagonist Tolerability Study-Heart Failure (ARTS-HF): a randomized study of finerenone vs. eplerenone in patients who have worsening chronic heart failure with diabetes and/or chronic kidney disease. Eur J Heart Fail. 2015 Feb;17(2):224-32. doi: 10.1002/ejhf.218. PubMed PMID: 25678098.
11: Ruilope LM, Agarwal R, Chan JC, Cooper ME, Gansevoort RT, Haller H, Remuzzi G, Rossing P, Schmieder RE, Nowack C, Ferreira AC, Pieper A, Kimmeskamp-Kirschbaum N, Bakris GL. Rationale, design, and baseline characteristics of ARTS-DN: a randomized study to assess the safety and efficacy of finerenone in patients with type 2 diabetes mellitus and a clinical diagnosis of diabetic nephropathy. Am J Nephrol. 2014;40(6):572-81. doi: 10.1159/000371497. Epub 2015 Jan 10. PubMed PMID: 25591469.
12: Miller RJ, Howlett JG. Evolving role for mineralocorticoid receptor antagonists in heart failure with preserved ejection fraction. Curr Opin Cardiol. 2015 Jan 8. [Epub ahead of print] PubMed PMID: 25574896.
13: Lother A, Moser M, Bode C, Feldman RD, Hein L. Mineralocorticoids in the heart and vasculature: new insights for old hormones. Annu Rev Pharmacol Toxicol. 2015;55:289-312. doi: 10.1146/annurev-pharmtox-010814-124302. Epub 2014 Sep 10. Review. PubMed PMID: 25251996.
14: Kolkhof P, Delbeck M, Kretschmer A, Steinke W, Hartmann E, Bärfacker L, Eitner F, Albrecht-Küpper B, Schäfer S. Finerenone, a novel selective nonsteroidal mineralocorticoid receptor antagonist protects from rat cardiorenal injury. J Cardiovasc Pharmacol. 2014 Jul;64(1):69-78. doi: 10.1097/FJC.0000000000000091. PubMed PMID: 24621652.
15: Bauersachs J. The ARTS of third-generation mineralocorticoid receptor antagonists: achieving cardiovascular benefit with minimized renal side effects? Eur Heart J. 2013 Aug;34(31):2426-8. doi: 10.1093/eurheartj/eht235. Epub 2013 Jul 3. PubMed PMID: 23824829.
16: Pitt B, Kober L, Ponikowski P, Gheorghiade M, Filippatos G, Krum H, Nowack C, Kolkhof P, Kim SY, Zannad F. Safety and tolerability of the novel non-steroidal mineralocorticoid receptor antagonist BAY 94-8862 in patients with chronic heart failure and mild or moderate chronic kidney disease: a randomized, double-blind trial. Eur Heart J. 2013 Aug;34(31):2453-63. doi: 10.1093/eurheartj/eht187. Epub 2013 May 27. PubMed PMID: 23713082; PubMed Central PMCID: PMC3743070.
17: Bärfacker L, Kuhl A, Hillisch A, Grosser R, Figueroa-Pérez S, Heckroth H, Nitsche A, Ergüden JK, Gielen-Haertwig H, Schlemmer KH, Mittendorf J, Paulsen H, Platzek J, Kolkhof P. Discovery of BAY 94-8862: a nonsteroidal antagonist of the mineralocorticoid receptor for the treatment of cardiorenal diseases. ChemMedChem. 2012 Aug;7(8):1385-403. doi: 10.1002/cmdc.201200081. Epub 2012 Jul 12. PubMed PMID: 22791416.
18: Pitt B, Filippatos G, Gheorghiade M, Kober L, Krum H, Ponikowski P, Nowack C, Kolkhof P, Kim SY, Zannad F. Rationale and design of ARTS: a randomized, double-blind study of BAY 94-8862 in patients with chronic heart failure and mild or moderate chronic kidney disease. Eur J Heart Fail. 2012 Jun;14(6):668-75. doi: 10.1093/eurjhf/hfs061. Epub 2012 May 4. PubMed PMID: 22562554.
