| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Targets |
Rentiapril primarily targets angiotensin-converting enzyme (ACE), a key enzyme in the renin-angiotensin-aldosterone system (RAAS). ACE is responsible for the conversion of angiotensin I to the potent vasoconstrictor angiotensin II. Rentiapril acts as a competitive inhibitor of ACE, binding to the enzyme's active site and preventing the conversion of angiotensin I to angiotensin II. By inhibiting ACE, Rentiapril reduces the levels of angiotensin II, leading to vasodilation, decreased peripheral vascular resistance, and reduced blood pressure. The compound's specificity for ACE over other peptidases contributes to its antihypertensive activity. Rentiapril is an orally active inhibitor, making it suitable for administration via the oral route in research studies.
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| ln Vitro |
Rentiapril demonstrates potent in vitro inhibitory activity against angiotensin-converting enzyme (ACE). As a competitive inhibitor, Rentiapril binds to the active site of ACE and blocks the conversion of angiotensin I to angiotensin II. The compound's inhibitory activity has been characterized in enzymatic assays using purified ACE and synthetic substrates. Rentiapril's ability to inhibit ACE activity in vitro correlates with its antihypertensive effects in vivo. The compound's potency and selectivity for ACE make it a valuable tool for studying the renin-angiotensin-aldosterone system and its role in cardiovascular and renal physiology. Rentiapril is an orally active compound, indicating good bioavailability when administered via the oral route.
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| ln Vivo |
Rentiapril has demonstrated in vivo antihypertensive activity as an orally active ACE inhibitor. By competitively binding to and inhibiting ACE, Rentiapril blocks the conversion of angiotensin I to angiotensin II, preventing the potent vasoconstrictive actions of angiotensin II and resulting in vasodilation. The compound's antihypertensive effects have been studied in animal models of hypertension. Additionally, Rentiapril has been evaluated in reproductive toxicity studies. The compound's oral bioavailability and in vivo efficacy make it a useful tool for cardiovascular and renal research. However, detailed reports of specific in vivo studies, including dosing regimens and outcome measures, are limited in the available literature.
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| Enzyme Assay |
The in vitro enzyme/receptor binding assay for Rentiapril typically involves measuring its inhibitory activity against angiotensin-converting enzyme (ACE) using enzymatic activity assays. The assay system includes purified ACE (from rabbit lung or other sources), a suitable peptide substrate (such as hippuryl-histidyl-leucine or Abz-Gly-p-nitro-Phe-Pro-OH), and assay buffer (typically containing Tris-HCl, sodium chloride, and zinc chloride at physiological pH). Rentiapril is added at varying concentrations (typically 0.1 nM to 100 uM) and pre-incubated with the enzyme before substrate addition. The reaction is incubated at 37degC for 30-60 minutes, and the hydrolysis of the substrate is monitored by measuring the formation of hippuric acid (by HPLC or spectrophotometry) or by fluorescence detection. IC₅0 values are calculated from dose-response curves using nonlinear regression analysis.
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| Cell Assay |
The in vitro cell-based assay for Rentiapril involves culturing relevant cell lines that express ACE, such as endothelial cells (HUVECs) or ACE-transfected cells. Cells are typically seeded in multi-well plates and treated with varying concentrations of Rentiapril (typically 0.1-100 uM) for 1-24 hours in appropriate culture media at 37degC with 5% CO2. Following treatment, ACE activity in cell lysates or conditioned media is measured using fluorescent or colorimetric substrates. Alternatively, the compound's effects on angiotensin II production can be assessed by adding angiotensin I to the culture and measuring angiotensin II levels by ELISA. Cell viability is assessed using standard assays such as MTT or LDH release to ensure that observed effects are not due to cytotoxicity. The compound's effects on endothelial function and vascular reactivity can also be evaluated in vitro.
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| Animal Protocol |
In vivo animal studies for Rentiapril have been conducted to evaluate its antihypertensive activity and safety profile. Typical animal models include spontaneously hypertensive rats (SHR), renovascular hypertensive models, or normotensive animals. Rentiapril is administered via oral gavage at doses typically ranging from 0.1-10 mg/kg, given daily or twice daily for 1-4 weeks. Common endpoints include systolic and diastolic blood pressure measurements (using tail-cuff or telemetry), heart rate, and plasma renin activity. Additionally, renal function parameters such as urinary protein excretion, glomerular filtration rate, and electrolyte balance are assessed. Reproductive toxicity studies have also been conducted. Histological analysis of cardiovascular and renal tissues is performed to assess target organ protection.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Rentiapril have been characterized to some extent. As an orally active compound, Rentiapril is orally bioavailable. The compound has a molecular weight of 368.47 g/mol and a molecular formula of C22H2₈N2O3. Its chemical structure is 4-hydroxy-3-methoxy-N-[2-[2-(1-methylpiperidin-2-yl)ethyl]phenyl]benzamide. The compound is soluble in DMSO and has a purity of ≥95%. However, detailed pharmacokinetic parameters such as half-life, Cmax, AUC, and bioavailability have not been extensively reported in the available literature. As an ACE inhibitor, Rentiapril's pharmacokinetic profile is likely similar to other drugs in this class, with good oral absorption and renal elimination.
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| Toxicity/Toxicokinetics |
Rentiapril (CAS#: 80830-42-8) is a research-grade ACE inhibitor with the molecular formula C22H2₈N2O3 and a molecular weight of 368.47. Also known as SA-446, Rentiapril is a potent, orally active angiotensin-converting enzyme (ACE) inhibitor with well-defined antihypertensive activity. The compound competitively binds to and inhibits ACE, blocking the conversion of angiotensin I to angiotensin II, preventing the potent vasoconstrictive actions of angiotensin II, and resulting in vasodilation. Rentiapril is a useful tool for cardiovascular and renal research and has been studied in reproductive toxicity studies. The compound has a purity of ≥95% and is intended for research purposes only. No clinical trials or regulatory approvals have been reported for Rentiapril.
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| References | |
| Additional Infomation |
Rentiapril is a potent angiotensin-converting enzyme (ACE) inhibitor with antihypertensive effects. Rentiapril competitively binds to and inhibits ACE activity, thereby blocking the conversion of angiotensin I to angiotensin II. This inhibits the potent vasoconstrictive effect of angiotensin II, leading to vasodilation. Rentiapril also reduces adrenal cortex aldosterone secretion for angiotensin II, thereby increasing sodium excretion and consequently increasing water excretion.
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| Molecular Formula |
C13H15NO4S2
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| Molecular Weight |
313.39300
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| Exact Mass |
313.044
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| CAS # |
80830-42-8
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| Related CAS # |
Rentiapril racemate;72679-47-1
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| PubChem CID |
71244
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| Appearance |
White to off-white solid powder
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| Density |
1.451g/cm3
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| Boiling Point |
553.7ºC at 760 mmHg
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| Flash Point |
288.7ºC
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| Index of Refraction |
1.66
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| LogP |
1.677
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
20
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| Complexity |
379
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| Defined Atom Stereocenter Count |
2
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| SMILES |
C1[C@H](N([C@H](S1)C2=CC=CC=C2O)C(=O)CCS)C(=O)O
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| InChi Key |
BSHDUMDXSRLRBI-JOYOIKCWSA-N
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| InChi Code |
InChI=1S/C13H15NO4S2/c15-10-4-2-1-3-8(10)12-14(11(16)5-6-19)9(7-20-12)13(17)18/h1-4,9,12,15,19H,5-7H2,(H,17,18)/t9-,12+/m0/s1
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| Chemical Name |
(2R,4R)-2-(2-hydroxyphenyl)-3-(3-sulfanylpropanoyl)-1,3-thiazolidine-4-carboxylic acid
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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 Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| 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 : ~200 mg/mL (~638.18 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (15.95 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 50.0 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: ≥ 5 mg/mL (15.95 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 50.0 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: ≥ 5 mg/mL (15.95 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 | 3.1909 mL | 15.9546 mL | 31.9091 mL | |
| 5 mM | 0.6382 mL | 3.1909 mL | 6.3818 mL | |
| 10 mM | 0.3191 mL | 1.5955 mL | 3.1909 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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