| Size | Price | Stock | Qty |
|---|---|---|---|
| 500mg |
|
||
| Other Sizes |
| Targets |
Canrenoate potassium targets the mineralocorticoid receptor (MR) through its active metabolite canrenone. The compound is a prodrug that is enzymatically converted in the body to canrenone, which is a potent competitive antagonist of the mineralocorticoid receptor. By blocking the mineralocorticoid receptor, the compound inhibits the effects of aldosterone, leading to increased sodium and water excretion and potassium retention. This diuretic action makes it useful in the treatment of hypertension and other conditions associated with fluid retention.
|
|---|---|
| ln Vitro |
In vitro, canrenoate potassium itself is relatively inactive as it requires enzymatic conversion to canrenone for activity. Canrenone, the active metabolite, is a potent competitive mineralocorticoid receptor antagonist. It binds to the mineralocorticoid receptor with high affinity and blocks aldosterone-mediated transcriptional activation. The compound's activity is typically assessed in cell-based reporter assays using mineralocorticoid response element (MRE)-luciferase constructs and by measuring the expression of aldosterone-responsive genes. Its diuretic effects are evaluated in functional assays measuring electrolyte transport in appropriate cell models.
|
| ln Vivo |
It has been demonstrated that potassium canrenoate increases myelogenous leukemia in rats in a dose-dependent manner and statistically significant increases malignant tumors of the brain, liver, thyroid, and mammary gland[2][3]. Rats' isoprenaline-induced cardiac fibrosis is reduced by potassium canrenoate (20 mg/kg/day; drinking water)[4].
In vivo, canrenoate potassium functions as a prodrug that is converted to the active metabolite canrenone. Canrenone is a potent competitive mineralocorticoid receptor antagonist that exerts diuretic effects by blocking aldosterone-mediated sodium reabsorption in the kidney. The compound is used as a diuretic for the treatment of hypertension. Its effects include increased sodium and water excretion with potassium retention. The compound's duration of action and efficacy depend on the rate of conversion to canrenone and the pharmacokinetic properties of the active metabolite. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays for canrenoate potassium typically involve the use of its active metabolite canrenone. Competitive binding experiments using mineralocorticoid receptor and radiolabeled or fluorescently labeled aldosterone as tracer are employed to assess binding affinity. Canrenone's binding affinity to the mineralocorticoid receptor is determined, with IC₅₀ or Kd values established. Assays are conducted in buffered solutions at physiological pH with appropriate receptor preparations. The compound's antagonist activity is confirmed through functional assays measuring MR-mediated transcriptional inhibition using MRE-luciferase reporter constructs.
|
| Cell Assay |
In vitro cell-based assays for canrenoate potassium typically involve the use of its active metabolite canrenone. Cell lines expressing mineralocorticoid receptor are treated with varying concentrations of canrenone for 24-48 hours. MR-mediated transcriptional activity is evaluated using reporter gene assays with MRE-luciferase constructs. The compound's antagonist activity is assessed by its ability to inhibit aldosterone-induced transcriptional activation. Standard cell culture conditions (37°C, 5% CO₂) with appropriate media are employed. Dose-response curves are generated to determine IC₅₀ values.
|
| Animal Protocol |
In vivo animal studies with canrenoate potassium typically involve administration of the compound to rodent models to evaluate its diuretic and antihypertensive effects. The compound is converted to canrenone in vivo, which then exerts mineralocorticoid receptor antagonist activity. Typical study designs include models of hypertension or fluid retention. Endpoints include measurements of blood pressure, urine output, electrolyte excretion, and plasma renin activity. The compound's effects on aldosterone-mediated sodium reabsorption in the kidney are evaluated. All procedures must comply with institutional animal care and use guidelines.
|
| ADME/Pharmacokinetics |
Canrenoate potassium has a molecular weight of 396.56 g/mol and a molecular formula of C₂₂H₂₉KO₄. It is very soluble in water and alcohol but insoluble in chloroform and ether. The compound is a prodrug that releases canrenone, the active mineralocorticoid receptor antagonist. It is used as a diuretic for hypertension treatment. The compound is typically stored at room temperature. Its pharmacokinetic properties are influenced by the rate of conversion to canrenone and the distribution of the active metabolite.
|
| Toxicity/Toxicokinetics |
Canrenoate potassium is approved for use as a diuretic in the treatment of hypertension. As an approved pharmaceutical agent, it has undergone comprehensive toxicological evaluation. Common adverse effects may include hyperkalemia, gastrointestinal disturbances, and electrolyte imbalances. The compound should be used with caution in patients with renal impairment or those taking other medications that affect potassium levels. Patients should be monitored for electrolyte imbalances and renal function. The compound should not be used in individuals with known hypersensitivity.
|
| References | |
| Additional Infomation |
A synthetic pregnadiene derivative with anti-aldosterone activity.
See also: canlinoic acid (note moved to). Canrenoate potassium (CAS#: 2181-04-6) has a molecular formula of C₂₂H₂₉KO₄ and a molecular weight of 396.56 g/mol. Its synonyms include potassium canrenoate, Aldadiene potassium, and SC-14266. It is a synthetic pregnadiene derivative with anti-aldosterone activity. Canrenoate potassium is a prodrug that releases canrenone, a potent competitive mineralocorticoid receptor antagonist. It is used as a diuretic for hypertension. It is very soluble in water. This compound has been approved for therapeutic use in certain regions. |
| Molecular Formula |
C22H29KO4
|
|---|---|
| Molecular Weight |
396.56
|
| Exact Mass |
396.17
|
| CAS # |
2181-04-6
|
| Related CAS # |
4138-96-9 (acid)
|
| PubChem CID |
23671691
|
| Appearance |
Light yellow to yellow solid powder
|
| LogP |
2.555
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
27
|
| Complexity |
713
|
| Defined Atom Stereocenter Count |
6
|
| SMILES |
C[C@]12CCC(=O)C=C1C=C[C@@H]3[C@@H]2CC[C@]4([C@H]3CC[C@]4(CCC(=O)[O-])O)C.[K+]
|
| InChi Key |
JTZQCHFUGHIPDF-RYVBEKKQSA-M
|
| InChi Code |
InChI=1S/C22H30O4.K/c1-20-9-5-15(23)13-14(20)3-4-16-17(20)6-10-21(2)18(16)7-11-22(21,26)12-8-19(24)25;/h3-4,13,16-18,26H,5-12H2,1-2H3,(H,24,25);/q;+1/p-1/t16-,17+,18+,20+,21+,22-;/m1./s1
|
| Chemical Name |
potassium;3-[(8R,9S,10R,13S,14S,17R)-17-hydroxy-10,13-dimethyl-3-oxo-2,8,9,11,12,14,15,16-octahydro-1H-cyclopenta[a]phenanthren-17-yl]propanoate
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
H2O: 100 mg/mL (252.17 mM)
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5217 mL | 12.6084 mL | 25.2169 mL | |
| 5 mM | 0.5043 mL | 2.5217 mL | 5.0434 mL | |
| 10 mM | 0.2522 mL | 1.2608 mL | 2.5217 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.
Link: https://clinicaltrials.gov/ct2/show/NCT04977960
Conditions:COVID-19 Acute Respiratory Distress SyndromeLink: https://clinicaltrials.gov/ct2/show/NCT04912011
Conditions:COVID-19 PneumoniaLink: https://www.clinicaltrialsregister.eu/ctr-search/search?query=2009-017464-17
Condition:Arterial hypertension associated with elevated ARR
Title:Blocage des effets létaux de l'aldostérone dans l'infarctus du myocarde traité ou non par la reperfusion pour améliorer le pronostic et la survie à six mois : Etude randomisée comparant un blocage spécifique de l'aldostérone en plus du traitement usuel au traitement usuel seul débuté dans les 72 premières heures après la survenue d'un infarctus aigu du myocarde'ALBATROSS'
Status:Ongoing
Date:2009-12-04
Eudractnumber:2008-006857-42
Link: https://www.clinicaltrialsregister.eu/ctr-search/search?query=2008-006857-42
Condition:InfractusProducts are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
