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| 10g |
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| 25g |
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Indapamide (Natrilix, Noranat, Fludex, Tertensif) is a potent thiazide-like diuretic used in the treatment of hypertension, as well as decompensated cardiac failure.
| 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].
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| 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].
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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). |
| References | |
| Additional Infomation |
Pharmacodynamics
Classified as a sulfonamide diuretic, indapamide is an effective antihypertensive agent and by extension, has shown efficacy in the prevention of target organ damage. Administration of indapamide produces water and electrolyte loss, with higher doses associated with increased diuresis. Severe and clinically significant electrolyte disturbances may occur with indapamide use - for example, hypokalemia resulting from renal potassium loss may lead to QTc prolongation. Further electrolyte imbalances may occur due to renal excretion of sodium, chloride, and magnesium. Other indapamide induced changes include increases in plasma renin and aldosterone, and reduced calcium excretion in the urine. In many studies investigating the effects of indapamide in both non-diabetic and diabetic hypertensive patients, glucose tolerance was not significantly altered. However, additional studies are necessary to assess the long term metabolic impacts of indapamide, since thiazide related impaired glucose tolerance can take several years to develop in non-diabetic patients. |
| 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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| 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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| 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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