产品
编 号：F231052
分子式：C20H18FN3O5
分子量：399.37
分子式：C20H18FN3O5
分子量：399.37
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规格
价格
是否有货
10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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50mg
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结构图
CAS No: 1850385-64-6
产品详情
生物活性：
Balcinrenone (AZD9977) is a potent, selective, and orally active mineralocorticoid receptor (MR) modulator. Balcinrenone is used for heart failure, and chronic kidney disease research.
体内研究：
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.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.Animal Model:Uni-nephrectomised male Sprague Dawley rats administered aldosterone and fed a high-salt diet with AZD9977
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
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.
体外研究：
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.
Balcinrenone (AZD9977) is a potent, selective, and orally active mineralocorticoid receptor (MR) modulator. Balcinrenone is used for heart failure, and chronic kidney disease research.
体内研究：
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.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.Animal Model:Uni-nephrectomised male Sprague Dawley rats administered aldosterone and fed a high-salt diet with AZD9977
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
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.
体外研究：
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.
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