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| | AZD9977 Basic information |
| Product Name: | AZD9977 | | Synonyms: | AZD9977;AZD9977,Inhibitor,T2DM,AZD-9977,Mineralocorticoid Receptor,Chronic Kidney Disease,?type 2 diabetes mellitus,inhibit,Heart Failure;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, 10 mM in DMSO;Balcinrenone;(3S)-4-[(3,4-Dihydro-3-oxo-2H-1,4-benzoxazin-6-yl)carbonyl]-7-fluoro-3,4-dihydro-N-methyl-2H-1,4-benzoxazine-3-acetamide (ACI) | | CAS: | 1850385-64-6 | | MF: | C20H18FN3O5 | | MW: | 399.37 | | EINECS: | | | Product Categories: | | | Mol File: | 1850385-64-6.mol |  |
| | AZD9977 Chemical Properties |
| 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 |
| | AZD9977 Usage And Synthesis |
| 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 |
| | AZD9977 Preparation Products And Raw materials |
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