WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H327003
CAS#: 945966-46-1
Description: Apararenone, also known as MT-3995, is a selective aldosterone receptor antagonist developed by Mitsubishi Tanabe Pharma, for the treatment of diabetic nephropathy. The compound is thought to reduce renal tissue damage by preventing proteinuria.
Hodoodo Cat#: H327003
Name: Apararenone
CAS#: 945966-46-1
Chemical Formula: C17H17FN2O4S
Exact Mass: 364.09
Molecular Weight: 364.391
Elemental Analysis: C, 56.04; H, 4.70; F, 5.21; N, 7.69; O, 17.56; S, 8.80
Synonym: MT-3995; MT 3995; MT3995; Apararenone
IUPAC/Chemical Name: N-(4-(4-fluorophenyl)-2,2-dimethyl-3-oxo-3,4-dihydro-2H-benzo[b][1,4]oxazin-7-yl)methanesulfonamide
InChi Key: AZNHWXAFPBYFGH-UHFFFAOYSA-N
InChi Code: InChI=1S/C17H17FN2O4S/c1-17(2)16(21)20(13-7-4-11(18)5-8-13)14-9-6-12(10-15(14)24-17)19-25(3,22)23/h4-10,19H,1-3H3
SMILES Code: CS(=O)(NC1=CC=C2N(C3=CC=C(F)C=C3)C(C(C)(C)OC2=C1)=O)=O
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
| Biological target: | |
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The following data is based on the product molecular weight 364.39 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
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2: Jiang X, Zhang Z, Li C, Zhang S, Su Q, Yang S, Liu X, Hu Y, Pu X. Efficacy and Safety of Non-Steroidal Mineralocorticoid Receptor Antagonists in Patients With Chronic Kidney Disease and Type 2 Diabetes: A Systematic Review Incorporating an Indirect Comparisons Meta-Analysis. Front Pharmacol. 2022 Jun 16;13:896947. doi: 10.3389/fphar.2022.896947. PMID: 35784710; PMCID: PMC9243561.
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4: Wada T, Inagaki M, Yoshinari T, Terata R, Totsuka N, Gotou M, Hashimoto G. Apararenone in patients with diabetic nephropathy: results of a randomized, double-blind, placebo-controlled phase 2 dose-response study and open-label extension study. Clin Exp Nephrol. 2021 Feb;25(2):120-130. doi: 10.1007/s10157-020-01963-z. Epub 2020 Sep 24. PMID: 32974732; PMCID: PMC7880964.
5: Okanoue T, Sakamoto M, Harada K, Inagaki M, Totsuka N, Hashimoto G, Kumada H. Efficacy and safety of apararenone (MT-3995) in patients with nonalcoholic steatohepatitis: A randomized controlled study. Hepatol Res. 2021 Sep;51(9):943-956. doi: 10.1111/hepr.13695. Epub 2021 Aug 5. PMID: 34260795.
6: Iijima T, Katoh M, Takedomi K, Yamamoto Y, Akatsuka H, Shirata N, Nishi A, Takakuwa M, Watanabe Y, Munakata H, Koyama N, Ikeda T, Iguchi T, Kato H, Kikkawa K, Kawaguchi T. Discovery of Apararenone (MT-3995) as a Highly Selective, Potent, and Novel Nonsteroidal Mineralocorticoid Receptor Antagonist. J Med Chem. 2022 Jun 23;65(12):8127-8143. doi: 10.1021/acs.jmedchem.2c00402. Epub 2022 Jun 2. PMID: 35652647.
7: Nakamura T, Shimizu H, Kawaguchi A. Drug-Drug Interactions of the Nonsteroidal Mineralocorticoid Receptor Antagonist Apararenone With Midazolam, Warfarin, and Digoxin: A Phase 1 Studies in Healthy Volunteers. Clin Ther. 2020 Nov;42(11):2171-2183.e4. doi: 10.1016/j.clinthera.2020.09.002. Epub 2020 Nov 3. PMID: 33153727.
8: Nakamura T, Kawaguchi A. Phase 1 Studies to Define the Safety, Tolerability, and Pharmacokinetic and Pharmacodynamic Profiles of the Nonsteroidal Mineralocorticoid Receptor Antagonist Apararenone in Healthy Volunteers. Clin Pharmacol Drug Dev. 2021 Apr;10(4):353-365. doi: 10.1002/cpdd.855. Epub 2020 Aug 20. PMID: 32820619; PMCID: PMC8048531.
9: Kolkhof P, Joseph A, Kintscher U. Nonsteroidal mineralocorticoid receptor antagonism for cardiovascular and renal disorders - New perspectives for combination therapy. Pharmacol Res. 2021 Oct;172:105859. doi: 10.1016/j.phrs.2021.105859. Epub 2021 Aug 28. PMID: 34461222.
10: Wu Y, Lin H, Tao Y, Xu Y, Chen J, Jia Y, Zheng Z. Network meta-analysis of mineralocorticoid receptor antagonists for diabetic kidney disease. Front Pharmacol. 2022 Sep 16;13:967317. doi: 10.3389/fphar.2022.967317. PMID: 36188560; PMCID: PMC9523214.
11: Vodošek Hojs N, Bevc S, Ekart R, Piko N, Petreski T, Hojs R. Mineralocorticoid Receptor Antagonists in Diabetic Kidney Disease. Pharmaceuticals (Basel). 2021 Jun 11;14(6):561. doi: 10.3390/ph14060561. PMID: 34208285; PMCID: PMC8230766.
12: Capelli I, Gasperoni L, Ruggeri M, Donati G, Baraldi O, Sorrenti G, Caletti MT, Aiello V, Cianciolo G, La Manna G. New mineralocorticoid receptor antagonists: update on their use in chronic kidney disease and heart failure. J Nephrol. 2020 Feb;33(1):37-48. doi: 10.1007/s40620-019-00600-7. Epub 2019 Apr 15. PMID: 30989614.
13: Yao L, Liang X, Wang P. Therapeutic perspective: evolving evidence of nonsteroidal mineralocorticoid receptor antagonists in diabetic kidney disease. Am J Physiol Endocrinol Metab. 2023 Jun 1;324(6):E531-E541. doi: 10.1152/ajpendo.00022.2023. Epub 2023 May 11. PMID: 37166263.
14: Kolkhof P, Bärfacker L. 30 YEARS OF THE MINERALOCORTICOID RECEPTOR: Mineralocorticoid receptor antagonists: 60 years of research and development. J Endocrinol. 2017 Jul;234(1):T125-T140. doi: 10.1530/JOE-16-0600. PMID: 28634268; PMCID: PMC5488394.
