ChemicalBook Product Catalog API Hormones and the Endocrine System Adrenal corticosteroids AZD9977

AZD9977

Product NameAZD9977
CAS1850385-64-6
MFC20H18FN3O5
MW399.37
EINECS
MOL File1850385-64-6.mol

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

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

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