| Identification | Back Directory | [Name]
AZD9977 | [CAS]
1850385-64-6 | [Synonyms]
AZD9977
Balcinrenone
2H-1,4-Benzoxazine-3-acetamide, 4-[(3,4-dihydro-3-oxo-2H-1,4-benzoxazin-6-yl)carbonyl]-7-fluoro-3,4-dihydro-N-methyl-, (3S)-
AZD9977,Inhibitor,T2DM,AZD-9977,Mineralocorticoid Receptor,Chronic Kidney Disease,?type 2 diabetes mellitus,inhibit,Heart Failure | [Molecular Formula]
C20H18FN3O5 | [MOL File]
1850385-64-6.mol | [Molecular Weight]
399.37 |
| Chemical Properties | Back Directory | [Boiling point ]
731.4±60.0 °C(Predicted) | [density ]
1.377±0.06 g/cm3(Predicted) | [solubility ]
DMSO : 250 mg/mL (625.99 mM; Need ultrasonic) | [form ]
Solid | [pka]
12.07±0.20(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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 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]. | 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. |
| [References]
[1] Fredrik Erlandsson, et al. Clinical safety, tolerability, pharmacokinetics and effects on urinary electrolyte excretion of AZD9977, a novel, selective mineralocorticoid receptor modulator. Br J Clin Pharmacol. 2018 Jul;84(7):1486-1493. DOI:10.1111/bcp.13562 |
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