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Apararenone

Cat. No. M21053
Apararenone Structure
Synonym:

MT-3995

Size Price Availability Quantity
5mg USD 150  USD150 In stock
10mg USD 250  USD250 In stock
25mg USD 425  USD425 In stock
50mg USD 750  USD750 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
Biological Activity

Apararenone is an oral nonsteroidal mineralocorticoid receptor (MR) antagonist.

Chemical Information
Molecular Weight 364.39
Formula C17H17FN2O4S
CAS Number 945966-46-1
Solubility (25°C) DMSO ≥ 100 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] Toru Iijima, et al. J Med Chem. Discovery of Apararenone (MT-3995) as a Highly Selective, Potent, and Novel Nonsteroidal Mineralocorticoid Receptor Antagonist

[2] Ulrich Kintscher, et al. Br J Pharmacol. Novel non-steroidal mineralocorticoid receptor antagonists in cardiorenal disease

[3] Takeshi Okanoue, et al. Hepatol Res. Efficacy and safety of apararenone (MT-3995) in patients with nonalcoholic steatohepatitis: A randomized controlled study

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

[5] Takashi Wada, et al. Clin Exp Nephrol. Apararenone in patients with diabetic nephropathy: results of a randomized, double-blind, placebo-controlled phase 2 dose-response study and open-label extension study

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Keywords: Apararenone, MT-3995 supplier, Mineralocorticoid Receptor, inhibitors, activators


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