Eplerenone | Inspra | CGP-30083 | CAS#107724-20-9 | Selective Aldosterone Receptor Antagonist

Eplerenone
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 328919

CAS#: 107724-20-9

Description: Eplerenone, also known as Inspra and CGP-30083, is a selective aldosterone receptor antagonist used to treat hypertension and congestive heart failure. Eplerenone provides marked protection against vascular injury in the kidney and heart.

Chemical Structure

Eplerenone

CAS# 107724-20-9

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 328919
Name: Eplerenone
CAS#: 107724-20-9
Chemical Formula: C24H30O6
Exact Mass: 414.20
Molecular Weight: 414.498
Elemental Analysis: C, 69.55; H, 7.30; O, 23.16

Price and Availability

Size	Price	Availability
10mg	USD 265	2 Weeks
25mg	USD 480	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: Eplerenone; CGP-30083; SC-66110; CGP 30083; SC 66110; CGP30083; SC66110; Inspra; Selara

IUPAC/Chemical Name: methyl (4aS,4bR,5aR,6aS,7R,9aS,9bR,10R)-4a,6a-dimethyl-2,5'-dioxo-2,4,4a,4',5a,5',6,6a,8,9,9a,9b,10,11-tetradecahydro-3H,3'H-spiro[cyclopenta[1,2]phenanthro[4,4a-b]oxirene-7,2'-furan]-10-carboxylate

InChi Key: JUKPWJGBANNWMW-VWBFHTRKSA-N

InChi Code: 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

SMILES Code: C[C@]12CCC(C=C1C[C@@H](C(OC)=O)[C@@H]3[C@]24[C@@H](C[C@@]5(C)[C@H]3CC[C@@]56CCC(O6)=O)O4)=O

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

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:

Product Data:

Product Data

Instruction:

View handling instruction

Biological target:	Eplerenone (Epoxymexrenone) is a selective, competitive and oreally active aldosterone antagonist with an IC50 of 138 nM.
In vitro activity:	Additionally, notably elevated Ki67 expression was observed in ox-LDL-stimulated VSMCs relative to the untreated group, whereas EPL (eplerenone) intervention significantly decreased Ki67 expression, especially under co-treatment with 3 μM EPL (Fig. 1C). Consistently, EPL markedly downregulated the expression of minichromosome maintenance-2 (MCM-2) and proliferating cell nuclear antigen (PCNA), which are key proliferation-related proteins, in ox-LDL-exposed VSMCs (Fig. 1D). These results implicate that EPL attenuates proliferation of VSMCs stimulated by ox-LDL. Reference: Adv Clin Exp Med. 2021 Apr;30(4):405-412. https://pubmed.ncbi.nlm.nih.gov/33915037/
In vivo activity:	To induce pulmonary hypertension, mice were exposed to chronic hypoxia for 6 weeks. Treatment with the MR antagonist eplerenone attenuated pulmonary vascular remodeling, hypertension, and right ventricular dysfunction. Reference: Hypertension. 2021 Aug;78(2):456-465. https://pubmed.ncbi.nlm.nih.gov/33966455/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMF	2.0	4.83
	DMF:PBS (pH 7.2) (1:1)	0.5	1.21

Preparing Stock Solutions

The following data is based on the product molecular weight 414.50 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:	1. Wang D, Wang M, Sun P, Gao Q. Eplerenone inhibits oxidized low-density lipoprotein-induced proliferation and migration of vascular smooth muscle cells by downregulating GPER expression. Adv Clin Exp Med. 2021 Apr;30(4):405-412. doi: 10.17219/acem/133484. PMID: 33915037. 2. Du L, Qin M, Yi Y, Chen X, Jiang W, Zhou L, Zhang D, Xu K, Yang Y, Li C, Liu Y, Liu X, Duan SZ. Eplerenone Prevents Atrial Fibrosis via the TGF-β Signaling Pathway. Cardiology. 2017;138(1):55-62. doi: 10.1159/000471918. Epub 2017 Jun 2. PMID: 28571007.epl 3. Kowalski J, Deng L, Suennen C, Koca D, Meral D, Bode C, Hein L, Lother A. Eplerenone Improves Pulmonary Vascular Remodeling and Hypertension by Inhibition of the Mineralocorticoid Receptor in Endothelial Cells. Hypertension. 2021 Aug;78(2):456-465. doi: 10.1161/HYPERTENSIONAHA.120.16196. Epub 2021 May 10. PMID: 33966455. 4. Xiong Y, Chang Y, Hao J, Zhang C, Yang F, Wang Z, Liu Y, Wang X, Mu S, Xu Q. Eplerenone Attenuates Fibrosis in the Contralateral Kidney of UUO Rats by Preventing Macrophage-to-Myofibroblast Transition. Front Pharmacol. 2021 Feb 24;12:620433. doi: 10.3389/fphar.2021.620433. PMID: 33716747; PMCID: PMC7943730.
In vitro protocol:	1. Wang D, Wang M, Sun P, Gao Q. Eplerenone inhibits oxidized low-density lipoprotein-induced proliferation and migration of vascular smooth muscle cells by downregulating GPER expression. Adv Clin Exp Med. 2021 Apr;30(4):405-412. doi: 10.17219/acem/133484. PMID: 33915037. 2. Du L, Qin M, Yi Y, Chen X, Jiang W, Zhou L, Zhang D, Xu K, Yang Y, Li C, Liu Y, Liu X, Duan SZ. Eplerenone Prevents Atrial Fibrosis via the TGF-β Signaling Pathway. Cardiology. 2017;138(1):55-62. doi: 10.1159/000471918. Epub 2017 Jun 2. PMID: 28571007.epl
In vivo protocol:	1. Kowalski J, Deng L, Suennen C, Koca D, Meral D, Bode C, Hein L, Lother A. Eplerenone Improves Pulmonary Vascular Remodeling and Hypertension by Inhibition of the Mineralocorticoid Receptor in Endothelial Cells. Hypertension. 2021 Aug;78(2):456-465. doi: 10.1161/HYPERTENSIONAHA.120.16196. Epub 2021 May 10. PMID: 33966455. 2. Xiong Y, Chang Y, Hao J, Zhang C, Yang F, Wang Z, Liu Y, Wang X, Mu S, Xu Q. Eplerenone Attenuates Fibrosis in the Contralateral Kidney of UUO Rats by Preventing Macrophage-to-Myofibroblast Transition. Front Pharmacol. 2021 Feb 24;12:620433. doi: 10.3389/fphar.2021.620433. PMID: 33716747; PMCID: PMC7943730.

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1: Struthers A, Krum H, Williams GH. A comparison of the aldosterone-blocking agents eplerenone and spironolactone. Clin Cardiol. 2008 Apr;31(4):153-8. doi: 10.1002/clc.20324. PMID: 18404673; PMCID: PMC6652937.

2: Provenzano M, Puchades MJ, Garofalo C, Jongs N, D'Marco L, Andreucci M, De Nicola L, Gorriz JL, Heerspink HJL; ROTATE-3 study group; ROTATE-3 study group members. Albuminuria-Lowering Effect of Dapagliflozin, Eplerenone, and Their Combination in Patients with Chronic Kidney Disease: A Randomized Crossover Clinical Trial. J Am Soc Nephrol. 2022 Aug;33(8):1569-1580. doi: 10.1681/ASN.2022020207. Epub 2022 Apr 19. PMID: 35440501; PMCID: PMC9342643.

3: Filippatos G, Anker SD, Böhm M, Gheorghiade M, Køber L, Krum H, Maggioni AP, Ponikowski P, Voors AA, Zannad F, Kim SY, Nowack C, Palombo G, Kolkhof P, Kimmeskamp-Kirschbaum N, Pieper A, Pitt B. A randomized controlled study of finerenone vs. eplerenone in patients with worsening chronic heart failure and diabetes mellitus and/or chronic kidney disease. Eur Heart J. 2016 Jul 14;37(27):2105-14. doi: 10.1093/eurheartj/ehw132. Epub 2016 Apr 29. PMID: 27130705; PMCID: PMC4946749.

4: Brown R, Quirk J, Kirkpatrick P. Eplerenone. Nat Rev Drug Discov. 2003 Mar;2(3):177-8. doi: 10.1038/nrd1039. PMID: 12619638.

5: Tam TS, Wu MH, Masson SC, Tsang MP, Stabler SN, Kinkade A, Tung A, Tejani AM. Eplerenone for hypertension. Cochrane Database Syst Rev. 2017 Feb 28;2(2):CD008996. doi: 10.1002/14651858.CD008996.pub2. PMID: 28245343; PMCID: PMC6464701.

6: Ito S, Itoh H, Rakugi H, Okuda Y, Yoshimura M, Yamakawa S. Double-Blind Randomized Phase 3 Study Comparing Esaxerenone (CS-3150) and Eplerenone in Patients With Essential Hypertension (ESAX-HTN Study). Hypertension. 2020 Jan;75(1):51-58. doi: 10.1161/HYPERTENSIONAHA.119.13569. Epub 2019 Dec 2. PMID: 31786983.

7: Burgess E. Eplerenone in hypertension. Expert Opin Pharmacother. 2004 Dec;5(12):2573-81. doi: 10.1517/14656566.5.12.2573. PMID: 15571474.

8: Abdelhakeem E, El-Nabarawi M, Shamma R. Eplerenone repurposing in management of chorioretinopathy: Mechanism, nanomedicine-based delivery applications and future trends. Br J Clin Pharmacol. 2022 Jun;88(6):2665-2672. doi: 10.1111/bcp.15213. Epub 2022 Feb 3. PMID: 34983084.

9: Manolis AA, Manolis TA, Melita H, Manolis AS. Eplerenone Versus Spironolactone in Resistant Hypertension: an Efficacy and/or Cost or Just a Men's Issue? Curr Hypertens Rep. 2019 Mar 2;21(3):22. doi: 10.1007/s11906-019-0924-0. PMID: 30826898.

10: Sehgal R, Singh H, Singh IP. Comparative study of spironolactone and eplerenone in management of ascites in patients of cirrhosis of liver. Eur J Gastroenterol Hepatol. 2020 Apr;32(4):535-539. doi: 10.1097/MEG.0000000000001678. PMID: 32044820.

11: Eplerenone after myocardial infarction? Drug Ther Bull. 2008 Jan;46(1):1-3. doi: 10.1136/dtb.2007.12.0006. PMID: 18171726.

12: Kobayashi M, Ferreira JP, Matsue Y, Chikamori T, Ito S, Asakura M, Yamashina A, Kitakaze M. Effect of eplerenone on clinical stability of Japanese patients with acute heart failure. Int J Cardiol. 2023 Mar 1;374:73-78. doi: 10.1016/j.ijcard.2022.12.045. Epub 2022 Dec 28. PMID: 36586516.

13: Stewart Coats AJ, Shewan L. Eplerenone's role in the management of complex cardiovascular disorders. Int J Cardiol. 2015 Dec 1;200:1-2. doi: 10.1016/j.ijcard.2015.05.128. Epub 2015 May 21. PMID: 26116081.

14: Liew D, Martin J, Krum H. Eplerenone. Pharmacia. Curr Opin Investig Drugs. 2003 Mar;4(3):316-22. PMID: 12744223.

15: Moore TD, Nawarskas JJ, Anderson JR. Eplerenone: a selective aldosterone receptor antagonist for hypertension and heart failure. Heart Dis. 2003 Sep- Oct;5(5):354-63. doi: 10.1097/01.hdx.0000089783.30450.cb. PMID: 14503934.

16: Barnes BJ, Howard PA. Eplerenone: a selective aldosterone receptor antagonist for patients with heart failure. Ann Pharmacother. 2005 Jan;39(1):68-76. doi: 10.1345/aph.1E306. Epub 2004 Dec 8. Erratum in: Ann Pharmacother. 2005 May;39(5):978. PMID: 15590870.

17: Brennan BJ, Martin NE. Eplerenone: selective aldosterone antagonism in management of cardiovascular and renal disease. J Am Pharm Assoc (2003). 2004 Sep-Oct;44(5):604-10; quiz 610-1. doi: 10.1331/1544-3191.44.5.604.brennan. PMID: 15496047.

18: Eplerenone (Inspra). Med Lett Drugs Ther. 2003 May 12;45(1156):39-40. PMID: 12736599.

19: Weinberger MH. Eplerenone: a new selective aldosterone receptor antagonist. Drugs Today (Barc). 2004 Jun;40(6):481-5. doi: 10.1358/dot.2004.40.6.850481. PMID: 15349128.

20: Sacconi R, Borrelli E, Querques G. Eplerenone for chronic central serous chorioretinopathy. Lancet. 2020 Nov 14;396(10262):1556. doi: 10.1016/S0140-6736(20)31610-X. PMID: 33189168.

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