(R)-Balcinrenone
Based on 1 Customer Validation
(R)-Balcinrenone ((R)-AZD9977) is an isomer of Balcinrenone (HY-120274). Balcinrenone is an orally active mineralocorticoid receptor modulator. Balcinrenone regulates mineralocorticoid receptor activity, inhibits aldosterone-induced target gene expression, and suppresses the activities of renal Toll-like receptor 4, MyD88 and NF-κB. Balcinrenone alleviates renal extracellular matrix remodeling, inflammatory cell infiltration, and the expression of renal injury markers. Balcinrenone restores myocardial perfusion reserve, regulates potassium homeostasis, and induces fecal potassium excretion. Balcinrenone is applicable to research on metabolism-related chronic kidney disease and heart failure.
For research use only. We do not sell to patients.
- Purity: 99.95%
- CAS No.: 1850385-65-7
- Formula: C20H18FN3O5
- Molecular Weight:399.37
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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TLR4 |
NF-κB |
IL-6 |
(R)-Balcinrenone is an isomer of Balcinrenone (HY-120274). Balcinrenone (0.1-12.5 μM) concentration-dependently inhibits the expression of MR target genes and cardiac injury/inflammatory markers in Aldosterone (HY-113313)-induced H9C2/MR+ rat cardiomyocytes; in the absence of Aldosterone, it partially upregulates Sgk-1[2] at higher concentrations.
(R)-Balcinrenone is an isomer of Balcinrenone. Balcinrenone inhibits aldosterone-induced fibrosis and inflammatory processes in primary human cardiac fibroblasts in a concentration-dependent manner, with complete inhibition of IL-6 at 0.5 μM and complete inhibition of type Ⅰ collagen at 12.5 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
(R)-Balcinrenone is an isomer of Balcinrenone. Balcinrenone (10-100 mg/kg/day; administered via feed mixing; daily dosing; for 24 consecutive weeks) restores myocardial perfusion reserve to the level of healthy mice and attenuates diet-induced perivascular cardiac fibrosis in male C57BL/6J mice with heart failure with preserved ejection fraction (HFpEF)[2].
(R)-Balcinrenone is an isomer of Balcinrenone. Balcinrenone (100 mg/kg; p.o.; twice daily for 4 consecutive days, with an additional single dose on day 5; total 5 days) does not increase plasma potassium levels in male CKD mice subjected to overnight potassium loading stimulation; instead, it enhances fecal potassium excretion[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57Bl7J (8-week-old male, 25-26 g, 5/6 nephrectomy + 8 weeks 60% high-fat diet induced CKD)[1]
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Dosage:100 mg/kg
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Administration:p.o.; daily; 8 weeks
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Result:Increased hematocrit to 29.6%.
Attenuated the decrease in hemoglobin to 10.1 g/dL.
Reduced plasma Na+ to 150.4 mM.
Increased plasma K+ to 4.6 mM.
Prevented the increase in Lcn2 expression.
Attenuated increased renal collagen deposition and reduced Col1a1 and Col3 mRNA levels.
Blunted increased renal deposition of biglycan, syndecan-1, and versican; fully prevented increased syndecan-1 and versican protein levels, partially decreased biglycan protein levels; decreased syndecan-1 and versican mRNA levels.
Blunted increased renal TLR4 immunostaining and reduced TLR4 mRNA levels.
Prevented increased MyD88 protein and mRNA expression.
Reduced the ratio of phosphorylated vs total NFκB.
Reduced CD68+ macrophage infiltration and protein expression; reduced CD3+ and CD4+ lymphocyte protein expression; prevented the up-regulation of CD68, CD3, and CD4 mRNA levels.
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Animal Model:C57BL/6J (male, 6 weeks old at study start, diet-induced model)[2]
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Dosage:10 mg/kg/day; 30 mg/kg/day; 100 mg/kg/day
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Administration:diet admixture; daily; 24 weeks
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Result:Yielded a myocardial perfusion reserve (MPR) of 1.50 (0.99-fold vs. high-fat diet).
Yielded an MPR of 1.78 (1.17-fold vs. high-fat diet).
Yielded an MPR of 1.68 (1.11-fold vs. high-fat diet).
Attenuated diet-induced cardiac perivascular fibrosis.
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Animal Model:C57BL/6J (male, 12 weeks old at study start, 5/6 nephrectomy-induced model)[2]
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Dosage:100 mg/kg
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Administration:p.o.; twice daily for 4 days, once on day 5; 5 days
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Result:Resulted in plasma potassium levels similar to vehicle-treated CKD mice, and ~1.2 mM lower than eplerenone-treated CKD mice.
Left creatinine-normalized urinary potassium excretion prior to potassium challenge unaffected.
Elevated fecal potassium excretion compared with vehicle-treated CKD mice.
Chemical Information
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CAS No. 1850385-65-7
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Appearance Solid
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Molecular Weight 399.37
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Formula C20H18FN3O5
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Color White to off-white
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SMILES
FC1=CC2=C(C=C1)N([C@@H](CO2)CC(NC)=O)C(C3=CC=C4OCC(NC4=C3)=O)=O
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Synonyms
(R)-AZD9977
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (250.39 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (281 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
[1]. Palacios-Ramirez R, et al. Mineralocorticoid receptor (MR) antagonist eplerenone and MR modulator balcinrenone prevent renal extracellular matrix remodeling and inflammation via the MR/proteoglycan/TLR4 pathway. Clinical science (London, England : 1979). 2024 Aug 21;138(16):1025-1038. [Content Brief]
[2]. Wolf MJ, et al. The novel mineralocorticoid receptor modulator balcinrenone protects against diet-induced cardiac microvascular dysfunction and plasma potassium elevation in mouse models. PloS one. 2026;21(2):e0341078. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.5039 mL | 12.5197 mL | 25.0394 mL | 62.5986 mL |
| 5 mM | 0.5008 mL | 2.5039 mL | 5.0079 mL | 12.5197 mL | |
| 10 mM | 0.2504 mL | 1.2520 mL | 2.5039 mL | 6.2599 mL | |
| 15 mM | 0.1669 mL | 0.8346 mL | 1.6693 mL | 4.1732 mL | |
| 20 mM | 0.1252 mL | 0.6260 mL | 1.2520 mL | 3.1299 mL | |
| 25 mM | 0.1002 mL | 0.5008 mL | 1.0016 mL | 2.5039 mL | |
| 30 mM | 0.0835 mL | 0.4173 mL | 0.8346 mL | 2.0866 mL | |
| 40 mM | 0.0626 mL | 0.3130 mL | 0.6260 mL | 1.5650 mL | |
| 50 mM | 0.0501 mL | 0.2504 mL | 0.5008 mL | 1.2520 mL | |
| 60 mM | 0.0417 mL | 0.2087 mL | 0.4173 mL | 1.0433 mL | |
| 80 mM | 0.0313 mL | 0.1565 mL | 0.3130 mL | 0.7825 mL | |
| 100 mM | 0.0250 mL | 0.1252 mL | 0.2504 mL | 0.6260 mL |
(R)-Balcinrenone Related Classifications
HY-120274A Related Classifications
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- (R)-Balcinrenone
- 1850385-65-7
- (R)-AZD9977
- Drug Isomer
- Mineralocorticoid Receptor
- Toll-like Receptor (TLR)
- NF-κB
- Interleukin Related
- Toll-like receptor 4
- H9C2/MR+ rat cardiomyocytes
- chronic kidney disease
- male C57BL/6J mice
- heart failure with preserved ejection fraction
- mineralocorticoid receptor
- aldosterone
- primary human cardiac fibroblasts
- MyD88
- Inhibitor
- inhibitor
- inhibit