| Size | Price | Stock | Qty |
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| 10g |
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| 25g |
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| 50g |
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| 100g |
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| Other Sizes |
| Targets |
Indapamide targets the Na⁺/Cl⁻ cotransporter (NCCT) in the distal convoluted tubule of the kidney. By inhibiting this transporter, it reduces sodium reabsorption, leading to increased urinary excretion of sodium, chloride, and water. It also blocks the slow component of the delayed rectifier potassium current (IKs) without altering the rapid component (IKr) or the inward rectifier current. Indapamide may also reduce responsiveness to pressor agents and decrease peripheral resistance.
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| ln Vitro |
In the isolated perfused rat pancreas, indapamide (0.1-500 mg/L; 20 minutes) decreases the total insulin secretory response to glucose infusion [2]. Indapamide (1-100 μM) inhibits bone resorption and promotes osteoblast growth [3].
In vitro, Indapamide acts as an inhibitor of the Na⁺/Cl⁻ cotransporter. Its diuretic and antihypertensive effects have been characterized in various experimental models. It is structurally and pharmacologically similar to thiazide diuretics. Interestingly, it is likely that thiazide-like diuretics such as indapamide have additional blood pressure lowering mechanisms that are unrelated to diuresis. |
| ln Vivo |
In spontaneously hypertensive rats (SHR), indapamide (1 mg/kg/d; gavage for 8 weeks) lowers blood pressure [4]. Rats that receive 10 mg/kg/d of indapamide had a decreased pressor response to oxytremorine, norepinephrine, and tyramine [1].
In vivo, Indapamide is an orally active antihypertensive and diuretic agent. It inhibits the reabsorption of sodium in the cortical dilution segment, increasing the urinary excretion of sodium and chlorides and, to a lesser extent, the excretion of potassium and magnesium. The antihypertensive effects of thiazides are sustained 4-6 weeks after initiation of therapy, despite recovering plasma and extracellular fluid volumes, suggesting additional mechanisms beyond diuresis. |
| Enzyme Assay |
The activity of Indapamide can be assessed using cell-free assays with isolated renal tubules or membrane preparations. The Na⁺/Cl⁻ cotransporter activity is measured by monitoring the uptake of radiolabeled sodium or chloride ions in the presence of varying concentrations of Indapamide. The IC₅₀ for inhibition of ion transport is determined from dose-response curves.
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| Cell Assay |
To evaluate the cellular effects of Indapamide, renal epithelial cells are treated with the compound. The inhibition of sodium and chloride transport is measured using ion-selective electrodes or fluorescent ion indicators. The effects on cell volume, membrane potential, and signaling pathways are assessed. The compound's effects on potassium channels can be evaluated using patch-clamp electrophysiology.
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| Animal Protocol |
Animal/Disease Models: Male spontaneously hypertensive rats (11 weeks) [4]
Doses: 1 mg/kg Route of Administration: Daily gavage for 8 weeks Experimental Results: Blood pressure diminished by 16.9 mm Hg. Increased dp/dtmax, ejection fraction (EF) and fractional shortening (FS). In vivo studies with Indapamide typically involve administration to animal models via oral routes. In models of hypertension, the compound's effects on blood pressure are assessed. Its diuretic effects are evaluated by measuring urine output and electrolyte excretion. In models of heart failure, its effects on edema and cardiac function are assessed. Pharmacokinetic parameters, such as bioavailability and half-life, are also characterized. |
| ADME/Pharmacokinetics |
Indapamide has a molecular formula of C₁₆H₁₆ClN₃O₃S and a molecular weight of 365.84 g/mol. Its CAS number is 26807-65-8. It is an oral antihypertensive agent. The compound should be stored according to the manufacturer's instructions.
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| Toxicity/Toxicokinetics |
Indapamide is generally well-tolerated but can cause side effects such as electrolyte imbalances (hypokalemia, hyponatremia), hyperglycemia, hyperuricemia, and dizziness. It is contraindicated in patients with anuria, severe renal impairment, or hypersensitivity to sulfonamides. It should be used with caution in patients with diabetes, gout, or liver disease.
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| References | |
| Additional Infomation |
Pharmacodynamics
Indapamide belongs to the sulfonamide diuretic class and is an effective antihypertensive drug that has been shown to prevent target organ damage. Administration of indapamide leads to water and electrolyte loss, with higher doses resulting in a stronger diuretic effect. Serious and clinically significant electrolyte disturbances can occur with indapamide use—for example, hypokalemia due to renal potassium loss can lead to QTc interval prolongation. Further electrolyte imbalances may occur due to renal excretion of sodium, chloride, and magnesium. Other changes caused by indapamide include elevated plasma renin and aldosterone levels, and decreased urinary calcium excretion. In many studies investigating the effects of indapamide on hypertensive patients with and without diabetes, glucose tolerance has not been significantly altered. However, further research is needed to assess the long-term metabolic effects of indapamide, as impaired glucose tolerance induced by thiazide derivatives may take several years to appear in non-diabetic patients. Indapamide is a thiazide-like diuretic and antihypertensive agent used for the treatment of hypertension and edema. It acts by inhibiting the Na⁺/Cl⁻ cotransporter in the distal convoluted tubule. Indapamide also has additional blood pressure lowering mechanisms unrelated to diuresis, such as reducing peripheral resistance. It is used as monotherapy or in combination with other antihypertensive agents. |
| Molecular Formula |
C16H16CLN3O3S
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|---|---|
| Molecular Weight |
365.8345
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| Exact Mass |
365.06
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| CAS # |
26807-65-8
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| Related CAS # |
(rac)-Indapamide-d3;1217052-38-4
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| PubChem CID |
3702
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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 |
160-162°C
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| Index of Refraction |
1.694
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| LogP |
2.1
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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 |
3
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| Heavy Atom Count |
24
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| Complexity |
580
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
NDDAHWYSQHTHNT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H16ClN3O3S/c1-10-8-11-4-2-3-5-14(11)20(10)19-16(21)12-6-7-13(17)15(9-12)24(18,22)23/h2-7,9-10H,8H2,1H3,(H,19,21)(H2,18,22,23)
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| Chemical Name |
4-chloro-N-(2-methyl-2,3-dihydroindol-1-yl)-3-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 : ≥ 100 mg/mL (~273.35 mM)
H2O : ~0.67 mg/mL (~1.83 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.83 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 25.0 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: ≥ 2.5 mg/mL (6.83 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 25.0 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: ≥ 2.5 mg/mL (6.83 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 | 2.7335 mL | 13.6676 mL | 27.3351 mL | |
| 5 mM | 0.5467 mL | 2.7335 mL | 5.4670 mL | |
| 10 mM | 0.2734 mL | 1.3668 mL | 2.7335 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.
Efficacy and Safety Study of the Fixed-dose Combination of Olmesartan + Indapamide When Compared to the Isolated Drugs in the Treatment of Hypertension.
CTID: NCT05110898
Phase: Phase 3 Status: Unknown status
Date: 2
Fixed-Dose Combination of Perindopril/Amlodipine (Amlessa®) and Fixed-Dose Combination of Perindopril/Indapamide /Amlodipine (Co-Amlessa®) - Contribution to Management in newly diagnosed and uncontrolled hypertensive patients (PRECIOUS study)
CTID: null
Phase: Phase 3 Status: Completed
Date: 2017-11-30
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