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MedKoo Cat#: 319580 | Name: Esaxerenone
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Description:

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

Esaxerenone, also known as CS-3150, XL-550, is a nonsteroidal antimineralocorticoid which was discovered by Exelixis and is now under development by Daiichi Sankyo Company for the treatment of hypertension, essential hypertension, hyperaldosteronism, and diabetic nephropathies. It acts as a highly selective silent antagonist of the mineralocorticoid receptor (MR), the receptor for aldosterone, with greater than 1,000-fold selectivity for this receptor over other steroid hormone receptors, and 4-fold and 76-fold higher affinity for the MR relative to the existing antimineralocorticoids spironolactone and eplerenone.

Chemical Structure

Esaxerenone
Esaxerenone
CAS#1632006-28-0

Theoretical Analysis

MedKoo Cat#: 319580

Name: Esaxerenone

CAS#: 1632006-28-0

Chemical Formula: C22H21F3N2O4S

Exact Mass: 466.1174

Molecular Weight: 466.48

Elemental Analysis: C, 56.65; H, 4.54; F, 12.22; N, 6.01; O, 13.72; S, 6.87

Price and Availability

Size Price Availability Quantity
5mg USD 150.00 Ready to ship
10mg USD 250.00 Ready to ship
25mg USD 450.00 Ready to ship
50mg USD 750.00 Ready to ship
100mg USD 1,350.00 Ready to ship
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Related CAS #
1632006-28-0 880780-76-7 1072195-82-4 (+ isomer) 1072195-83-5 (- isomer)
Synonym
Esaxerenone; CS-3150; CS 3150; CS3150; XL-550; XL550; XL 550.
IUPAC/Chemical Name
1-(2-hydroxyethyl)-4-methyl-N-(4-(methylsulfonyl)phenyl)-5-(2-(trifluoromethyl)phenyl)-1H-pyrrole-3-carboxamide
InChi Key
NOSNHVJANRODGR-UHFFFAOYSA-N
InChi Code
InChI=1S/C22H21F3N2O4S/c1-14-18(21(29)26-15-7-9-16(10-8-15)32(2,30)31)13-27(11-12-28)20(14)17-5-3-4-6-19(17)22(23,24)25/h3-10,13,28H,11-12H2,1-2H3,(H,26,29)
SMILES Code
CS(C1=CC=C(NC(C2=CN(CCO)C(C3=CC=CC=C3C(F)(F)F)=C2C)=O)C=C1)(=O)=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, 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
CAS# 880780-76-7; 1072195-82-4 (+ isomer); 1072195-83-5 (- isomer); 1632006-28-0 (5S isomer)
Biological target:
Esaxerenone (CS-3150) is a highly potent and selective non-steroidal mineralocorticoid receptor antagonist.
In vitro activity:
For example, as the rectangular voltage step from −80 to −10 mV with a duration of 40 ms was delivered (indicated in the inset of Figure 1A) to activate INa, the addition of 3 μM ESAX (esaxerenone) was noticed to result in an evident decrease in the peak or late amplitude of INa to 1104 ± 197 or 9 ± 1 pA (n = 8, p < 0.05) from control values of 1498 ± 241 or 19 ± 3 pA (n = 8), respectively. After removal of ESAX, the peak or late amplitude of the current returned to 1452 ± 228 or 18 ± 3 pA (n = 8, p < 0.05), respectively. Reference: Biomedicines. 2021 May; 9(5): 549. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8153305/
In vivo activity:
All HSD-fed DSS rats died by 24 weeks of age (18 weeks of HSD feeding), whereas 100% of the LSD-fed DSS rats were alive even at 28 weeks, suggesting that the HSD-fed rats exhibited a relatively shorter lifespan (Figure 1A). However, 20% of the HSD-fed rats with concomitant intervention of esaxerenone were alive at 28 weeks. Kaplan-Meier curve analysis of the cumulative probability of survival revealed that esaxerenone treatment significantly improved mean survival time in the HSD-fed DSS rats. Reference: Int J Mol Sci. 2021 Feb; 22(4): 2069. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7922950/
Solvent mg/mL mM
Solubility
DMSO 100.0 214.37
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 466.48 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.

Recalculate based on batch purity %
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. Chang WT, Wu SN. Characterization of Direct Perturbations on Voltage-Gated Sodium Current by Esaxerenone, a Nonsteroidal Mineralocorticoid Receptor Blocker. Biomedicines. 2021 May 13;9(5):549. doi: 10.3390/biomedicines9050549. PMID: 34068333; PMCID: PMC8153305. 2. Rahman A, Sawano T, Sen A, Hossain A, Jahan N, Kobara H, Masaki T, Kosaka S, Kitada K, Nakano D, Imamura T, Ohsaki H, Nishiyama A. Cardioprotective Effects of a Nonsteroidal Mineralocorticoid Receptor Blocker, Esaxerenone, in Dahl Salt-Sensitive Hypertensive Rats. Int J Mol Sci. 2021 Feb 19;22(4):2069. doi: 10.3390/ijms22042069. PMID: 33669786; PMCID: PMC7922950. 3. Bhuiyan AS, Rafiq K, Kobara H, Masaki T, Nakano D, Nishiyama A. Effect of a novel nonsteroidal selective mineralocorticoid receptor antagonist, esaxerenone (CS-3150), on blood pressure and renal injury in high salt-treated type 2 diabetic mice. Hypertens Res. 2019 Jun;42(6):892-902. doi: 10.1038/s41440-019-0211-0. Epub 2019 Jan 21. PMID: 30664703.
In vitro protocol:
1. Chang WT, Wu SN. Characterization of Direct Perturbations on Voltage-Gated Sodium Current by Esaxerenone, a Nonsteroidal Mineralocorticoid Receptor Blocker. Biomedicines. 2021 May 13;9(5):549. doi: 10.3390/biomedicines9050549. PMID: 34068333; PMCID: PMC8153305.
In vivo protocol:
1. Rahman A, Sawano T, Sen A, Hossain A, Jahan N, Kobara H, Masaki T, Kosaka S, Kitada K, Nakano D, Imamura T, Ohsaki H, Nishiyama A. Cardioprotective Effects of a Nonsteroidal Mineralocorticoid Receptor Blocker, Esaxerenone, in Dahl Salt-Sensitive Hypertensive Rats. Int J Mol Sci. 2021 Feb 19;22(4):2069. doi: 10.3390/ijms22042069. PMID: 33669786; PMCID: PMC7922950. 2. Bhuiyan AS, Rafiq K, Kobara H, Masaki T, Nakano D, Nishiyama A. Effect of a novel nonsteroidal selective mineralocorticoid receptor antagonist, esaxerenone (CS-3150), on blood pressure and renal injury in high salt-treated type 2 diabetic mice. Hypertens Res. 2019 Jun;42(6):892-902. doi: 10.1038/s41440-019-0211-0. Epub 2019 Jan 21. PMID: 30664703.
1: Wan N, Rahman A, Nishiyama A. Esaxerenone, a novel nonsteroidal mineralocorticoid receptor blocker (MRB) in hypertension and chronic kidney disease. J Hum Hypertens. 2021 Feb;35(2):148-156. doi: 10.1038/s41371-020-0377-6. Epub 2020 Jul 13. PMID: 32661269. 2: Ito S, Kashihara N, Shikata K, Nangaku M, Wada T, Okuda Y, Sawanobori T. Esaxerenone (CS-3150) in Patients with Type 2 Diabetes and Microalbuminuria (ESAX-DN): Phase 3 Randomized Controlled Clinical Trial. Clin J Am Soc Nephrol. 2020 Dec 7;15(12):1715-1727. doi: 10.2215/CJN.06870520. Epub 2020 Nov 25. PMID: 33239409; PMCID: PMC7769030. 3: 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. 4: Janković SM, Janković SV. Clinical Pharmacokinetics and Pharmacodynamics of Esaxerenone, a Novel Mineralocorticoid Receptor Antagonist: A Review. Eur J Drug Metab Pharmacokinet. 2022 May;47(3):291-308. doi: 10.1007/s13318-022-00760-1. Epub 2022 Feb 21. PMID: 35190999. 5: Qiang P, Hao J, Yang F, Han Y, Chang Y, Xian Y, Xiong Y, Gao X, Liang L, Shimosawa T, Xu Q. Esaxerenone inhibits the macrophage-to-myofibroblast transition through mineralocorticoid receptor/TGF-β1 pathway in mice induced with aldosterone. Front Immunol. 2022 Sep 6;13:948658. doi: 10.3389/fimmu.2022.948658. PMID: 36148244; PMCID: PMC9485811. 6: Uchida HA, Nakajima H, Hashimoto M, Nakamura A, Nunoue T, Murakami K, Hosoya T, Komoto K, Taguchi T, Akasaka T, Shiosakai K, Sugimoto K, Wada J; EX-DKD investigators. Efficacy and Safety of Esaxerenone in Hypertensive Patients with Diabetic Kidney Disease: A Multicenter, Open-Label, Prospective Study. Adv Ther. 2022 Nov;39(11):5158-5175. doi: 10.1007/s12325-022-02294-z. Epub 2022 Sep 7. PMID: 36070133; PMCID: PMC9449923. 7: Hoshide S. Is esaxerenone the ultimate mineralocorticoid receptor antagonist? Hypertens Res. 2023 Feb;46(2):516-517. doi: 10.1038/s41440-022-01056-2. Epub 2022 Oct 26. PMID: 36289363. 8: Morimoto S, Ichihara A. Efficacy of esaxerenone-a nonsteroidal mineralocorticoid receptor blocker-on nocturnal hypertension. Hypertens Res. 2022 Feb;45(2):376-377. doi: 10.1038/s41440-021-00803-1. Epub 2021 Nov 26. PMID: 34837032. 9: Bavuu O, Fukuda D, Ganbaatar B, Matsuura T, Ise T, Kusunose K, Yamaguchi K, Yagi S, Yamada H, Soeki T, Wakatsuki T, Sata M. Esaxerenone, a selective mineralocorticoid receptor blocker, improves insulin sensitivity in mice consuming high-fat diet. Eur J Pharmacol. 2022 Sep 15;931:175190. doi: 10.1016/j.ejphar.2022.175190. Epub 2022 Aug 9. PMID: 35961594. 10: Duggan S. Esaxerenone: First Global Approval. Drugs. 2019 Mar;79(4):477-481. doi: 10.1007/s40265-019-01073-5. PMID: 30806972. 11: Przezak A, Bielka W, Pawlik A. Hypertension and Type 2 Diabetes-The Novel Treatment Possibilities. Int J Mol Sci. 2022 Jun 10;23(12):6500. doi: 10.3390/ijms23126500. PMID: 35742943; PMCID: PMC9224227. 12: Yamamoto H, Yoshida N, Kihara S. Esaxerenone Blocks Vascular Endothelial Inflammation Through SGK1. J Cardiovasc Pharmacol. 2022 Oct 1;80(4):583-591. doi: 10.1097/FJC.0000000000001316. PMID: 35900901. 13: Rakugi H, Yamakawa S, Sugimoto K. Management of hyperkalemia during treatment with mineralocorticoid receptor blockers: findings from esaxerenone. Hypertens Res. 2021 Apr;44(4):371-385. doi: 10.1038/s41440-020-00569-y. Epub 2020 Nov 20. PMID: 33214722; PMCID: PMC8019656. 14: Fujimoto M, Watanabe S, Igarashi K, Ruike Y, Ishiwata K, Naito K, Ishida A, Koshizaka M, Suzuki S, Shiko Y, Koide H, Yokote K. Antihypertensive Effects of Esaxerenone in Older Patients with Primary Aldosteronism. Int J Hypertens. 2023 Jan 17;2023:6453933. doi: 10.1155/2023/6453933. PMID: 36704237; PMCID: PMC9873463. 15: Kirigaya Y, Shiramoto M, Ishizuka T, Uchimaru H, Irie S, Kato M, Shimizu T, Nakatsu T, Nishikawa Y, Ishizuka H. Pharmacokinetic interactions of esaxerenone with amlodipine and digoxin in healthy Japanese subjects. BMC Pharmacol Toxicol. 2020 Jul 29;21(1):55. doi: 10.1186/s40360-020-00423-4. PMID: 32727577; PMCID: PMC7389645. 16: Oshima A, Imamura T, Narang N, Kinugawa K. Renoprotective Effect of the Mineralocorticoid Receptor Antagonist Esaxerenone. Circ Rep. 2021 May 12;3(6):333-337. doi: 10.1253/circrep.CR-21-0024. PMID: 34136708; PMCID: PMC8180375. 17: Ito S, Itoh H, Rakugi H, Okuda Y, Iijima S. Antihypertensive effects and safety of esaxerenone in patients with moderate kidney dysfunction. Hypertens Res. 2021 May;44(5):489-497. doi: 10.1038/s41440-020-00585-y. Epub 2020 Dec 16. PMID: 33323991; PMCID: PMC8099724. 18: Pandey AK, Bhatt DL, Cosentino F, Marx N, Rotstein O, Pitt B, Pandey A, Butler J, Verma S. Non-steroidal mineralocorticoid receptor antagonists in cardiorenal disease. Eur Heart J. 2022 Aug 14;43(31):2931-2945. doi: 10.1093/eurheartj/ehac299. Erratum in: Eur Heart J. 2022 Nov 1;43(41):4391. PMID: 35713973. 19: Kintscher U, Bakris GL, Kolkhof P. Novel non-steroidal mineralocorticoid receptor antagonists in cardiorenal disease. Br J Pharmacol. 2022 Jul;179(13):3220-3234. doi: 10.1111/bph.15747. Epub 2022 Jan 13. PMID: 34811750. 20: Hattori M, Rahman A, Kidoguchi S, Jahan N, Fujisawa Y, Morisawa N, Ohsaki H, Kobara H, Masaki T, Hossain A, Steeve A, Nishiyama A. Association of Antihypertensive Effects of Esaxerenone with the Internal Sodium Balance in Dahl Salt-Sensitive Hypertensive Rats. Int J Mol Sci. 2022 Aug 10;23(16):8915. doi: 10.3390/ijms23168915. PMID: 36012182; PMCID: PMC9408866.