1. Metabolic Enzyme/Protease
  2. Mineralocorticoid Receptor
  3. AZD9977

AZD9977 

Cat. No.: HY-120274 Purity: 99.85%
Handling Instructions

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

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

AZD9977 Chemical Structure

AZD9977 Chemical Structure

CAS No. : 1850385-64-6

Size Price Stock Quantity
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
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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

In Vitro

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 AZD9977 with MR is characterized in a reporter gene assay where the full-length MR drives a luciferase reporter gene in U2-OS cells. AZD9977 antagonizes aldosterone-activated MR with an IC50 of 0.28 μM. Whereas eplerenone is a full antagonist, AZD9977 suppresses only 69% of the MR activity in this assay.
Species selective potencies of AZD9977 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

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. AZD9977 is as efficacious as full MR antagonists on renal protection, despite the partial antagonism observed in in vitro assays[1].
AZD9977 (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 provided by MCE.
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

AZD9977AZD 9977AZD-9977Mineralocorticoid ReceptorHeart FailureChronic Kidney Disease?type 2 diabetes mellitusT2DMmineralocorticoid receptorMRInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
AZD9977
Cat. No.:
HY-120274
Quantity:
MCE Japan Authorized Agent: