1. Metabolic Enzyme/Protease
  2. Mineralocorticoid Receptor
  3. Balcinrenone

Balcinrenone  (Synonyms: AZD9977)

Cat. No.: HY-120274 Purity: 99.85%
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Balcinrenone (AZD9977) is a potent, selective, and orally active mineralocorticoid receptor (MR) modulator. Balcinrenone is used for heart failure, and chronic kidney disease research.

For research use only. We do not sell to patients.

Balcinrenone Chemical Structure

Balcinrenone Chemical Structure

CAS No. : 1850385-64-6

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5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 580 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1100 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1700 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2500 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

Balcinrenone (AZD9977) is a potent, selective, and orally active mineralocorticoid receptor (MR) modulator. Balcinrenone is used for heart failure, and chronic kidney disease research[1].

In Vitro

Balcinrenone (AZD9977) and eplerenone activities on MR, GR, PR and AR in binding assays. The observed pKi of MR, GR, and PR are 7.5, 5.4 and 4.6, respectively.
Functional interaction of Balcinrenone with MR is characterized in a reporter gene assay where the full-length MR drives a luciferase reporter gene in U2-OS cells. Balcinrenone antagonizes aldosterone-activated MR with an IC50 of 0.28 μM. Whereas eplerenone is a full antagonist, Balcinrenone suppresses only 69% of the MR activity in this assay.
Species selective potencies of Balcinrenone are established in reporter gene assays using the MR LBDs from human, mouse or rat. The corresponding IC50 values are 0.37 μM, 0.08 μM and 0.08μM, respectively.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Balcinrenone (AZD9977) (oral administration; 10-100 mg/kg; 4 weeks) dose dependently reduces the UACR compared to vehicle in uni-nephrectomised male Sprague Dawley rats administered aldosterone and fed a high-salt diet. Balcinrenone is as efficacious as full MR antagonists on renal protection, despite the partial antagonism observed in in vitro assays[1].
Balcinrenone (oral administration; 100 mg/kg; co-administration with enalapril) stops further disease progression and reduces the urine albumin excretion (UAE) compared to vehicle treatment. Co-administration of enalapril has an apparent additive effect on UAE reduction, although this reduction is not statistically significant[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Uni-nephrectomised male Sprague Dawley rats administered aldosterone and fed a high-salt diet with AZD9977[1]
Dosage: 10, 30 and 100 mg/kg
Administration: Oral administration; 10-100 mg/kg; 4 weeks
Result: Improved kidney function and histology in animal models of CKD.
Animal Model: Db/db mice uni-nephrectomised at 8 weeks of age are treated from age 18w to age 22w[1]
Dosage: 100 mg/kg
Administration: Oral administration; 100 mg/kg; co-administration with enalapril
Result: Reduced albuminuria in diabetic kidney disease.
Co-administration of enalapril with AZD9977 had an additive effect on renal pathology scoring.
Clinical Trial
Molecular Weight

399.37

Formula

C20H18FN3O5

CAS No.
SMILES

FC1=CC2=C(N(C(C3=CC=C(OCC(N4)=O)C4=C3)=O)[[email protected]@H](CC(NC)=O)CO2)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (625.99 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5039 mL 12.5197 mL 25.0394 mL
5 mM 0.5008 mL 2.5039 mL 5.0079 mL
10 mM 0.2504 mL 1.2520 mL 2.5039 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.21 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (5.21 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (5.21 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Balcinrenone
Cat. No.:
HY-120274
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