| Size | Price | Stock | Qty |
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| 1mg |
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| 100mg | |||
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| Targets |
RPH-2823 functions as a basic triamterene derivative with diuretic activity. Triamterene is a potassium-sparing diuretic that acts by blocking epithelial sodium channels (ENaC) in the collecting ducts of the kidney. By inhibiting ENaC, RPH-2823 reduces sodium reabsorption and increases sodium excretion, which in turn decreases potassium excretion (potassium-sparing effect). The compound induces a dose-dependent decrease in short-circuit current (SCC), which is a measure of active ion transport across epithelial tissues, and an increase in transepithelial electrical resistance. These effects are consistent with inhibition of sodium channel-mediated ion transport. The compound's diuretic activity is attributed to its action on renal epithelial sodium channels.
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| ln Vitro |
RPH-2823 interacts with Na+ channels or their regulatory locations in the apical membrane to influence transepithelial Na+ transport [1].
In vitro, RPH-2823 induces a dose-dependent decrease in short-circuit current (SCC) and an increase in transepithelial electrical resistance in epithelial tissues. These effects indicate that the compound inhibits active ion transport across epithelial cell layers. The compound's effects have been characterized using Ussing chamber studies, which measure ion transport across epithelial tissues. The compound's mechanism of action is consistent with inhibition of epithelial sodium channels (ENaC). Its in vitro activity profile makes it a useful tool for studying ion transport mechanisms and diuretic pharmacology. |
| ln Vivo |
On male Wistar rats, the potassium excretion effect of 25 μmol/kg furosemide can be avoided by using RPH 2823 (2.5 μmol/kg). RPH 2823 has a 3-hour terminal elimination half-life when given intravenously at doses of 1 mg/kg and 5 mg/kg. A dosage is eliminated in the urine unaltered in around 47% of cases [2].
In vivo, RPH-2823 has diuretic activity, with sodium-sparing (potassium-sparing) effects. The compound induces a dose-dependent diuretic response. Pharmacokinetic studies have been performed to characterize its elimination and excretion. The compound's terminal half-life is 3 hours when given intravenously, and about 47% of the administered dose is excreted unchanged in urine. These properties make RPH-2823 a useful tool for studying diuretic mechanisms and ion transport in vivo. However, the compound has not been developed for clinical use. |
| Enzyme Assay |
For in vitro ion transport studies, RPH-2823 is evaluated using Ussing chamber techniques. Epithelial tissues (e.g., renal collecting duct cells, frog skin, or cultured epithelial monolayers) are mounted in Ussing chambers, and short-circuit current (SCC) and transepithelial resistance (TER) are measured. The compound is added to the apical or basolateral side of the tissue at various concentrations, and changes in SCC and TER are recorded. The dose-dependent decrease in SCC and increase in TER are quantified. For mechanism studies, the compound's effects are compared with those of known ENaC inhibitors such as amiloride or triamterene.
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| Cell Assay |
For in vitro cell-based assays, renal epithelial cell lines (e.g., MDCK, A6 cells) expressing ENaC are cultured on permeable supports and mounted in Ussing chambers or used in 96-well plate formats. Cells are treated with RPH-2823 at various concentrations, and transepithelial electrical resistance (TEER) is measured using a voltmeter. Sodium flux or short-circuit current is measured to assess ion transport. Cytotoxicity is assessed using MTT or LDH release assays. The compound's effects on ENaC expression and function can also be studied by Western blotting or patch-clamp electrophysiology.
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| Animal Protocol |
For in vivo animal studies, RPH-2823 is typically administered intravenously or orally. In models of diuretic activity, animals (e.g., rats, mice) are given the compound, and urine output, electrolyte excretion (Na⁺, K⁺, Cl⁻), and body weight are monitored. The compound's diuretic, natriuretic, and potassium-sparing effects are assessed. Pharmacokinetic studies are performed to determine drug concentrations in plasma and urine, and the elimination half-life and excretion profile are characterized.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of RPH-2823 have been characterized in animal studies. After intravenous administration at doses of 1 mg/kg and 5 mg/kg, the compound has a terminal half-life of 3 hours. Approximately 47% of the administered dose is excreted unchanged in the urine. The compound's distribution, metabolism, and oral bioavailability have not been extensively characterized. As a small molecule, it is expected to have reasonable tissue distribution.
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| Toxicity/Toxicokinetics |
Specific toxicity data for RPH-2823 are limited. The compound is used as a research tool and is not intended for human therapeutic use. As a diuretic, it may cause electrolyte imbalances at high doses. Standard laboratory safety precautions should be observed when handling the compound. Comprehensive toxicological studies have not been published.
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| References |
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| Additional Infomation |
RPH-2823 is a research compound with no clinical trial or regulatory approval status. It is a basic triamterene derivative used as a pharmacological tool to study ion transport and diuretic mechanisms. The compound's effects on short-circuit current and transepithelial resistance make it useful for studying ENaC function and regulation. It is commercially available from chemical suppliers for research purposes only. The compound is not used as a drug in clinical practice.
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| Molecular Formula |
C17H22N8O2
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|---|---|
| Molecular Weight |
370.40898
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| Exact Mass |
370.186
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| CAS # |
96558-24-6
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| PubChem CID |
125984
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
690.8±65.0 °C at 760 mmHg
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| Flash Point |
371.6±34.3 °C
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| Vapour Pressure |
0.0±2.3 mmHg at 25°C
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| Index of Refraction |
1.720
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| LogP |
0.47
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
27
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| Complexity |
462
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| Defined Atom Stereocenter Count |
0
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| SMILES |
OC(CN(C)C)COC1C=CC(C2C(N)=NC3N=C(N)N=C(C=3N=2)N)=CC=1
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| InChi Key |
DREYSFUKNSYCCL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H22N8O2/c1-25(2)7-10(26)8-27-11-5-3-9(4-6-11)12-14(18)22-16-13(21-12)15(19)23-17(20)24-16/h3-6,10,26H,7-8H2,1-2H3,(H6,18,19,20,22,23,24)
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| Chemical Name |
1-(dimethylamino)-3-[4-(2,4,7-triaminopteridin-6-yl)phenoxy]propan-2-ol
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| 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 | 2.6997 mL | 13.4986 mL | 26.9971 mL | |
| 5 mM | 0.5399 mL | 2.6997 mL | 5.3994 mL | |
| 10 mM | 0.2700 mL | 1.3499 mL | 2.6997 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.
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