AZD9977

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

Product information

CAS Number: 1850385-64-6

Molecular Weight: 399.37

Formula: C20H18FN3O5

Chemical Name: 2-[(3S)-7-fluoro-4-(3-oxo-3,4-dihydro-2H-1,4-benzoxazine-6-carbonyl)-3,4-dihydro-2H-1,4-benzoxazin-3-yl]-N-methylacetamide

Smiles: CNC(=O)C[C@H]1COC2C=C(F)C=CC=2N1C(=O)C1C=C2NC(=O)COC2=CC=1

InChiKey: MBKYLPOPYYLTNW-ZDUSSCGKSA-N

InChi: InChI=1S/C20H18FN3O5/c1-22-18(25)8-13-9-28-17-7-12(21)3-4-15(17)24(13)20(27)11-2-5-16-14(6-11)23-19(26)10-29-16/h2-7,13H,8-10H2,1H3,(H,22,25)(H,23,26)/t13-/m0/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

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

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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.

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. 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.

Products are for research use only. Not for human use.