| Bioactivity | 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]. | ||||||||||||
| Invitro | 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. | ||||||||||||
| 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: | ||||||||||||
| Name | Balcinrenone | ||||||||||||
| CAS | 1850385-64-6 | ||||||||||||
| Formula | C20H18FN3O5 | ||||||||||||
| Molar Mass | 399.37 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
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| Reference | [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. |
Balcinrenone
CAS: 1850385-64-6 F: C20H18FN3O5 W: 399.37
Balcinrenone (AZD9977) is a potent, selective, and orally active mineralocorticoid receptor (MR) modulator. Balcinrenone
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