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AZD9977

Cat. No. M11399
AZD9977  Structure
Synonym:

Balcinrenone

Size Price Availability Quantity
5mg USD 350  USD350 In stock
10mg USD 520  USD520 In stock
25mg USD 925  USD925 In stock
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Quality Control & Documentation
Biological Activity

AZD9977 is a potent, selective, and orally active modulator of corticosteroid receptors (MR). AZD9977 was studied for heart failure and chronic kidney disease.

Chemical Information
Molecular Weight 399.37
Formula C20H18FN3O5
CAS Number 1850385-64-6
Solubility (25°C) DMSO ≥ 200 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Christopher J Rush, et al. JAMA Cardiol. Prevalence of Coronary Artery Disease and Coronary Microvascular Dysfunction in Patients With Heart Failure With Preserved Ejection Fraction

[2] Vishal Patel, et al. Drug Dev Res. Role of mineralocorticoid receptor antagonists in kidney diseases

[3] Andrew Whittaker, et al. Clin Transl Sci. Safety, Tolerability, and Pharmacokinetics of the Mineralocorticoid Receptor Modulator AZD9977 in Healthy Men: A Phase I Multiple Ascending Dose Study

[4] Krister Bamberg, et al. J Renin Angiotensin Aldosterone Syst. The selective mineralocorticoid receptor modulator AZD9977 reveals differences in mineralocorticoid effects of aldosterone and fludrocortisone

[5] Krister Bamberg, et al. PLoS One. Preclinical pharmacology of AZD9977: A novel mineralocorticoid receptor modulator separating organ protection from effects on electrolyte excretion

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Keywords: AZD9977 , Balcinrenone supplier, Mineralocorticoid Receptor, inhibitors, activators


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