| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
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| 100mg |
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| Other Sizes |
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| ln Vitro |
In a dose-dependent way, canrenone suppresses the synthesis of aldosterone, corticosterone, 18-hydroxydeoxycorticosterone, and 18-hydroxycorticosterone [1]. The effects of canrenone on platelet-derived growth factor-induced cell motility and proliferation are dose-dependent. Na+/H+ exchanger 1 activity generated by platelet-derived growth factor is inhibited by canrenone [2].
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| ln Vivo |
The primary active metabolite of spironolactone in rats is canrenone, which has a short half-life. The effects of spironolactone and canrenone on RAAS vary with duration of treatment, suggesting that spironolactone is more effective and canrenone's antimineralocorticoid activity is diminished [3].
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| References |
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| Additional Infomation |
Canrenone is a steroid lactone.
Canrenone has been used in trials studying the diagnostic of Heart Failure. Canrenone is an aldosterone antagonist with potassium-sparing diuretic activity. Canrenone specifically antagonizes aldosterone at the mineralocorticoid receptor in the kidneys, thereby increasing sodium excretion and inhibiting potassium excretion. Canrenone is the primary active metabolite of both spironolactone and canreonate potassium. A synthetic pregnadiene compound with anti-aldosterone activity. |
| Molecular Formula |
C22H26O6
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|---|---|
| Molecular Weight |
386.44
|
| Exact Mass |
340.203
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| CAS # |
976-71-6
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| Related CAS # |
Canrenone-d6;Canrenone-d4
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| PubChem CID |
13789
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| Appearance |
White to light yellow solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
541.1±50.0 °C at 760 mmHg
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| Melting Point |
158-160ºC
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| Flash Point |
237.6±30.2 °C
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| Vapour Pressure |
0.0±1.4 mmHg at 25°C
|
| Index of Refraction |
1.581
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| LogP |
2.99
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
25
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| Complexity |
719
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| Defined Atom Stereocenter Count |
6
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| SMILES |
C[C@]12CC[C@@H]3[C@]4(CCC(=O)C=C4C=C[C@H]3[C@@H]1CC[C@]12CCC(=O)O1)C
|
| InChi Key |
UJVLDDZCTMKXJK-WNHSNXHDSA-N
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| InChi Code |
InChI=1S/C22H28O3/c1-20-9-5-15(23)13-14(20)3-4-16-17(20)6-10-21(2)18(16)7-11-22(21)12-8-19(24)25-22/h3-4,13,16-18H,5-12H2,1-2H3/t16-,17+,18+,20+,21+,22-/m1/s1
|
| Chemical Name |
(8R,9S,10R,13S,14S,17R)-10,13-dimethylspiro[2,8,9,11,12,14,15,16-octahydro-1H-cyclopenta[a]phenanthrene-17,5'-oxolane]-2',3-dione
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| Synonyms |
Aldadiene BRN-0046602 BRN 0046602
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 100 mg/mL (~293.72 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3 mg/mL (8.81 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 30.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 3 mg/mL (8.81 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 30.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 3 mg/mL (8.81 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5877 mL | 12.9386 mL | 25.8772 mL | |
| 5 mM | 0.5175 mL | 2.5877 mL | 5.1754 mL | |
| 10 mM | 0.2588 mL | 1.2939 mL | 2.5877 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03263962 | COMPLETED | Drug: Canrenone | Cardiac Heart Failure Patients | University of Pavia | 2017-07-13 | |
| NCT04977960 | UNKNOWN STATUS | Drug: Potassium Canrenoate | COVID-19 Acute Respiratory Distress Syndrome | Fondazione IRCCS Ca' Granda, Ospedale Maggiore Policlinico | 2022-09 | Phase 2 |
| NCT00403910 | COMPLETED | Drug: Canrenone | Heart Failure | Heart Care Foundation | 2002-09 | Phase 3 |
| NCT02687178 | COMPLETED | Drug: Canrenone 50 vs canrenone 100 mg | Essential Hypertension | University of Pavia | 2010-10 | Phase 4 |
| NCT03536806 | UNKNOWN STATUS | Drug: Saline 0.9% Drug: Canrenone |
Atrial Fibrillation, Paroxysmal | National Institute of Cardiology, Warsaw, Poland | 2018-06 | Phase 4 |
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