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Purity: ≥98%
Esaxerenone, formerly 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.
| ln Vivo |
The maximum plasma concentration (Cmax) and area under the plasma concentration versus time curve (AUC) increased with increasing dose after a single oral administration of 0.1, 0.3, 1, and 3 mg/kg esaxerenone. Esaxerenone's maximum plasma concentration (Tmax) can be reached in 2.0–4.5 hours. The systemic clearance (CL) and volume of distribution (Vss) at steady state following an intravenous injection of 0.1, 0.3, 1 and 3 mg/kg of esaxerenone were 3.53 to 6.69 mL/min/kg and 1.47 to 2.49 L/kg, respectively. Rats: 2.79 to 3.69 mL/min/kg; cynomolgus monkeys: 1.34 to 1.54 L/kg; and rats: 2.79 to 3.69 mL/min/kg. Rat urine and feces excreted 3.9% and 91.4%, respectively, of the dosed radioactive material within 168 hours of administration, for a total of 95.2%. In monkeys, 82.3% of the radioactive material expelled in feces and 11.5% in urine made up a total of 93.9% within 168 hours [1].
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| References |
[1]. Yamada M, et al. Pharmacokinetics, distribution, and disposition of esaxerenone, a novel, highly potent and selective non-steroidal mineralocorticoid receptor antagonist, in rats and monkeys. Xenobiotica. 2017 Dec;47(12):1090-1103
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| Molecular Formula |
C22H21F3N2O4S
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|---|---|
| Molecular Weight |
466.4752
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| Exact Mass |
466.1174
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| CAS # |
1632006-28-0
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| Related CAS # |
1632006-28-0;880780-76-7;1072195-82-4 (+ isomer);1072195-83-5 (- isomer);
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| SMILES |
CS(C1=CC=C(NC(C2=CN(CCO)C(C3=CC=CC=C3C(F)(F)F)=C2C)=O)C=C1)(=O)=O
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| InChi Key |
NOSNHVJANRODGR-UHFFFAOYSA-N
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| 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)
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| Chemical Name |
1-(2-hydroxyethyl)-4-methyl-N-(4-(methylsulfonyl)phenyl)-5-(2-(trifluoromethyl)phenyl)-1H-pyrrole-3-carboxamide
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| Synonyms |
Esaxerenone CS-3150 CS 3150 CS3150 XL-550 XL550 XL 550.
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~214.38 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.46 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.46 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: 2.08 mg/mL (4.46 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1437 mL | 10.7186 mL | 21.4371 mL | |
| 5 mM | 0.4287 mL | 2.1437 mL | 4.2874 mL | |
| 10 mM | 0.2144 mL | 1.0719 mL | 2.1437 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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