| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| Targets |
Thiazide-sensitive sodium-chloride cotransporter (NCC) in the distal convoluted tubule. Xipamide inhibits the sodium-chloride cotransporter, reducing sodium and chloride reabsorption. This leads to increased delivery of sodium and water to the distal segments, resulting in diuresis and decreased blood volume.
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| ln Vitro |
Xipamide demonstrates diuretic activity in vitro by inhibiting sodium and chloride transport in renal epithelial cells. The compound has been characterized in various in vitro assays using renal tubule preparations or cultured kidney cells. Its potency and efficacy have been compared to other thiazide and thiazide-like diuretics.
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| ln Vivo |
In vivo, Xipamide is used clinically for the treatment of hypertension and edema. It increases urine output and reduces blood pressure by promoting sodium and water excretion. The compound is effective as a monotherapy or in combination with other antihypertensive agents. Its diuretic effect is dose-dependent and sustained.
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| Enzyme Assay |
In vitro assays for Xipamide involve measuring sodium and chloride transport in renal epithelial cell lines or isolated renal tubules. Cells are treated with Xipamide at varying concentrations, and ion transport is measured using electrophysiological techniques or fluorescent indicators. The compound's inhibition of the sodium-chloride cotransporter is assessed.
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| Cell Assay |
Cellular assays for Xipamide involve culturing renal epithelial cells expressing the thiazide-sensitive sodium-chloride cotransporter. Cells are treated with Xipamide, and sodium uptake is measured using radiolabeled sodium or fluorescent sodium indicators. The compound's inhibitory effects on ion transport are assessed.
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| Animal Protocol |
In vivo animal studies for Xipamide are conducted in rodent models to assess its diuretic and antihypertensive effects. The compound is typically administered orally. Urine output, electrolyte excretion, and blood pressure are measured. Dosing regimens vary depending on the study. The compound has been studied in various hypertensive animal models.
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| ADME/Pharmacokinetics |
Xipamide is well absorbed after oral administration and has a long duration of action, allowing once-daily dosing. It is metabolized in the liver and excreted via the renal route. The compound is highly protein-bound and has a half-life of approximately 24 hours. Detailed pharmacokinetic parameters have been characterized in clinical studies.
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| Toxicity/Toxicokinetics |
Xipamide is generally well-tolerated but can cause side effects typical of diuretics, including electrolyte disturbances (hypokalemia, hyponatremia), dehydration, and hyperglycemia. It is contraindicated in patients with severe renal impairment, anuria, or hypersensitivity to sulfonamides. The compound should be used with caution in patients with hepatic impairment.
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| References | |
| Additional Infomation |
Xipamide belongs to the benzamide class of drugs. Xipamide is a sulfonamide diuretic. Xipamide acts on the distal convoluted tubule. In addition, it has a weak inhibitory effect on carbonic anhydrase (CA). It is a sulfonylbenzamide analog of clopamide. It has diuretic, hypotensive, and antihypertensive effects. It binds to plasma proteins, therefore its onset of action is slow and its duration of action is long.
Xipamide is a thiazide-like diuretic used for the treatment of hypertension and edema. It inhibits the sodium-chloride cotransporter in the distal convoluted tubule, promoting diuresis and reducing blood pressure. The compound is available as a prescription medication in many countries. It is also known by the brand name Diurexan. |
| Molecular Formula |
C15H15CLN2O4S
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|---|---|
| Molecular Weight |
354.8086
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| Exact Mass |
354.044
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| CAS # |
14293-44-8
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| PubChem CID |
26618
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Melting Point |
255-256ºC
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| Index of Refraction |
1.653
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| LogP |
2.5
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
23
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| Complexity |
526
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
MTZBBNMLMNBNJL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H15ClN2O4S/c1-8-4-3-5-9(2)14(8)18-15(20)10-6-13(23(17,21)22)11(16)7-12(10)19/h3-7,19H,1-2H3,(H,18,20)(H2,17,21,22)
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| Chemical Name |
4-chloro-N-(2,6-dimethylphenyl)-2-hydroxy-5-sulfamoylbenzamide
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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 : ~250 mg/mL (~704.60 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.86 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 20.8 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: ≥ 2.08 mg/mL (5.86 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 20.8 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: ≥ 2.08 mg/mL (5.86 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 | 2.8184 mL | 14.0920 mL | 28.1841 mL | |
| 5 mM | 0.5637 mL | 2.8184 mL | 5.6368 mL | |
| 10 mM | 0.2818 mL | 1.4092 mL | 2.8184 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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