| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg | |||
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| Other Sizes |
| Targets |
Chlorazanil exerts its pharmacological effect by selectively blocking sodium and chloride ion reabsorption in the distal renal tubule. It appears to inhibit the absorption of sodium and chloride in the distal convoluted tubule, promoting diuresis and modulating electrolyte balance without inducing significant systemic toxicity. Additionally, Chlorazanil increases renal prostaglandin activity by increased prostaglandin synthesis.
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| ln Vitro |
In vitro, Chlorazanil demonstrates diuretic activity by inhibiting sodium and chloride transport in renal tubular preparations. The compound has been studied for its effects on electrolyte transport in isolated renal tubules or cultured renal epithelial cells. It may also interfere with cytochrome P450 or other oxidase activities, affecting metabolic processes. Detailed in vitro activity data including specific IC50 values are limited in publicly available sources.
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| ln Vivo |
In vivo, Chlorazanil acts as an orally active diuretic that promotes urine output by blocking sodium and chloride reabsorption in the distal renal tubule. It has been shown to increase urinary excretion of sodium, chloride, and water without causing significant systemic toxicity. The compound modulates electrolyte balance and may have additional effects on renal prostaglandin activity. Its diuretic efficacy has been demonstrated in animal models and clinical studies.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for Chlorazanil typically involve measuring its effects on ion transport in renal tubular preparations or cultured renal epithelial cells. Sodium and chloride flux assays are performed using radioactive tracers (²²Na⁺ or ³⁶Cl⁻) or ion-selective electrodes. Cells or isolated tubules are incubated with varying concentrations of Chlorazanil, and the rate of ion uptake or efflux is measured. The degree of inhibition of ion transport is used to calculate IC50 values. Prostaglandin synthesis assays may also be performed to assess the compound's effects on renal prostaglandin production.
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| Cell Assay |
Cellular assays for Chlorazanil typically use renal epithelial cell lines (e.g., MDCK or LLC-PK1 cells) grown on permeable supports to form polarized monolayers. The cells are treated with Chlorazanil at various concentrations, and transepithelial electrical resistance (TEER) or short-circuit current (Isc) is measured to assess ion transport. Sodium and chloride flux across the monolayer is quantified using radioactive tracers or ion-selective electrodes. The degree of inhibition of ion transport is calculated from dose-response curves.
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| Animal Protocol |
In vivo animal studies for diuretic efficacy typically use rat or mouse models. Animals are administered Chlorazanil orally or intravenously at various doses, and urine is collected over a defined period (e.g., 4-24 hours). Urine volume, sodium concentration, chloride concentration, and potassium concentration are measured. The diuretic effect is expressed as increase in urine output and electrolyte excretion compared to vehicle-treated controls. Furosemide or hydrochlorothiazide may be used as positive controls.
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| ADME/Pharmacokinetics |
Chlorazanil is orally active with good bioavailability following oral administration. As a small-molecule diuretic, it is absorbed from the gastrointestinal tract and distributed to the kidneys where it exerts its pharmacological effect. The compound is metabolized in the liver, and its metabolites are excreted primarily via the kidneys. Detailed PK parameters such as half-life, Cmax, and AUC are not extensively published but are consistent with those of other triazine diuretics.
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| Toxicity/Toxicokinetics |
Chlorazanil is characterized as a low-toxicity diuretic that does not induce significant systemic toxicity at therapeutic doses. Preclinical toxicity studies indicate a favorable safety profile with no significant organ toxicity observed. The compound is well-tolerated in animal models and clinical use. Standard toxicity assessments would include acute toxicity in rodents, repeated-dose toxicity studies, and genotoxicity evaluations. Its low toxicity profile makes it a valuable agent for renal physiology research.
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| Additional Infomation |
Chlorazanil is a diamino-1,3,5-triazine compound. It is a triazine derivative and also a diuretic. Chlorazanil appears to inhibit the absorption of sodium and chloride in the distal convoluted tubule.
Chlorazanil is a triazine-derived diuretic that functions as a novel, orally active, and low-toxicity agent for promoting diuresis. It selectively blocks sodium and chloride reabsorption in the distal renal tubule, modulating electrolyte balance without significant systemic toxicity. Additionally, it increases renal prostaglandin activity through enhanced prostaglandin synthesis. The compound is used in renal physiology research and diuretic drug development. It is not approved for clinical use in most major markets but remains a research tool. |
| Molecular Formula |
C9H8CLN5
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|---|---|
| Molecular Weight |
221.64632
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| Exact Mass |
221.047
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| CAS # |
500-42-5
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| Related CAS # |
Chlorazanil hydrochloride;2019-25-2
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| PubChem CID |
10374
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.483g/cm3
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| Boiling Point |
457.2ºC at 760mmHg
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| Flash Point |
230.3ºC
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| Index of Refraction |
1.72
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| LogP |
2.505
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
15
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| Complexity |
195
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| Defined Atom Stereocenter Count |
0
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| SMILES |
NC1=NC=NC(NC2=CC=C(Cl)C=C2)=N1
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| InChi Key |
YRZQHIVOIFJEEE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C9H8ClN5/c10-6-1-3-7(4-2-6)14-9-13-5-12-8(11)15-9/h1-5H,(H3,11,12,13,14,15)
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| Chemical Name |
2-N-(4-chlorophenyl)-1,3,5-triazine-2,4-diamine
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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 : ~110 mg/mL (~496.28 mM)
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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 | 4.5116 mL | 22.5581 mL | 45.1162 mL | |
| 5 mM | 0.9023 mL | 4.5116 mL | 9.0232 mL | |
| 10 mM | 0.4512 mL | 2.2558 mL | 4.5116 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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