| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Na-Cl cotransporter (NCC) in the distal convoluted tubule (thiazide-like diuretic).
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|---|---|
| ln Vitro |
In the presence of 3-5 mM TEA, tripamide (less than 10 μg/ml) suppresses the spike generated by outward current pulses but does not change the membrane potential or resistance[1]. Tripamide reduces the amplitude of ejps elicited by perivascular nerve stimulation in the mesenteric artery. Tripamide, however, has less of an impact on the facilitation process brought about by repeated stimulation[1].
In vitro, Tripamide (<10 microg/ml) does not modify the membrane potential and resistance but suppresses the spike evoked by outward current pulses in the presence of TEA. In the mesenteric artery, it suppresses the amplitude of e.j.ps evoked by perivascular nerve stimulation. |
| ln Vivo |
Tripamide (0.6-160 mg/kg) increases urine volume and salt and chloride excretion in rats fed 25 ml/kg of normal saline orally in a dose-dependent manner. Rats' potassium excretion increased only when given a dosage of 160 mg/kg[2]. Tripamide has anti-hypertensive properties; when given to spontaneously hypertensive rats at a dose of 10 mg/kg/day for four weeks, the rats' potassium excretion rose by less than 50% while their urine volume doubled[2].
In rats loaded orally with 25 ml/kg of normal saline, Tripamide (0.6-160 mg/kg) increases urine volume and sodium and chloride excretion dose-dependently. At 160 mg/kg, it increases potassium excretion. In spontaneously hypertensive rats, 10 mg/kg/day for 4 weeks doubles urine volume and sodium excretion, while potassium excretion increases by <50%. |
| Enzyme Assay |
Tripamide's inhibition of the Na-Cl cotransporter (NCC) is typically assessed using radiolabeled substrate uptake assays in oocytes or cultured cells expressing the human NCC. The compound is incubated with the cells, and the uptake of 22Na+ or 36Cl- is measured.
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| Cell Assay |
Tripamide's diuretic effects are studied in primary cultures of human renal epithelial cells or immortalized distal tubule cells (e.g., HEK293 cells expressing NCC). The compound is added to the culture medium, and its effect on transepithelial ion transport is measured.
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| Animal Protocol |
In vivo, Tripamide is formulated in a suitable vehicle (e.g., 0.5% methylcellulose) and administered orally to rats (0.6-160 mg/kg). The animals are placed in metabolic cages, and urine volume, sodium, potassium, and chloride excretion are measured. Blood pressure is also monitored.
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| ADME/Pharmacokinetics |
Tripamide is well absorbed orally, with a plasma half-life suitable for once-daily dosing. It is metabolized in the liver and excreted in urine and feces. Its onset of action is relatively rapid, with peak effects observed within a few hours.
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| Toxicity/Toxicokinetics |
The acute toxicity of Tripamide is low. Common side effects include electrolyte imbalances (hypokalemia, hyponatremia), dehydration, and increased blood uric acid levels (hyperuricemia). It may also cause allergic reactions in sulfonamide-sensitive individuals.
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| References |
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| Additional Infomation |
Tripamide is an organic molecular entity.
Tripamide is an orally active diuretic used as an antihypertensive agent. It belongs to the sulfonamide class of diuretics and is structurally related to thiazide diuretics, such as hydrochlorothiazide. It is a research tool for studying renal function. |
| Molecular Formula |
C16H20CLN3O3S
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|---|---|
| Molecular Weight |
369.87
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| Exact Mass |
369.091
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| CAS # |
73803-48-2
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| PubChem CID |
5282210
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| Appearance |
White to off-white solid powder
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| Density |
1.51g/cm3
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| Index of Refraction |
1.673
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| LogP |
3.72
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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 |
605
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| Defined Atom Stereocenter Count |
4
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| SMILES |
C1CC2C[C@H]1[C@H]3[C@@H]2CN(C3)NC(=O)C4=CC(=C(C=C4)Cl)S(=O)(=O)N
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| InChi Key |
UHLOVGKIEARANS-FZMOHWGLSA-N
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| InChi Code |
InChI=1S/C16H20ClN3O3S/c17-14-4-3-11(6-15(14)24(18,22)23)16(21)19-20-7-12-9-1-2-10(5-9)13(12)8-20/h3-4,6,9-10,12-13H,1-2,5,7-8H2,(H,19,21)(H2,18,22,23)/t9-,10?,12-,13+/m0/s1
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| Chemical Name |
N-[(2R,6S,7S)-4-azatricyclo[5.2.1.02,6]decan-4-yl]-4-chloro-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) |
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 | 2.7037 mL | 13.5183 mL | 27.0365 mL | |
| 5 mM | 0.5407 mL | 2.7037 mL | 5.4073 mL | |
| 10 mM | 0.2704 mL | 1.3518 mL | 2.7037 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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