| Size | Price | Stock | Qty |
|---|---|---|---|
| 500mg |
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| 1g |
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| 2g |
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| 10g | |||
| Other Sizes |
Purity: ≥98%
| Targets |
Benazepril HCl targets angiotensin-converting enzyme (ACE). As a prodrug, it is metabolized to its active form, benazeprilat, which inhibits ACE. This prevents the conversion of angiotensin I to angiotensin II, a potent vasoconstrictor. By reducing angiotensin-II production, it leads to vasodilation and decreased blood pressure. It also inhibits oxidative stress and apoptosis through the PI3K/Akt signaling pathway.
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| ln Vitro |
Benazepril, an angiotensin converting enzyme inhibitor, which is a medication used to treat high blood pressure. Target: angiotensin converting enzyme (ACE) Benazepril is a medication used to treat high blood pressure (hypertension), congestive heart failure, and chronic renal failure. Upon cleavage of its ester group by the liver, benazepril is converted into its active form benazeprilat, a non-sulfhydryl angiotensin-converting enzyme (ACE) inhibitor.
In vitro, Benazepril HCl acts as an ACE inhibitor. By inhibiting ACE, it prevents the conversion of angiotensin I to angiotensin II. This leads to a decrease in angiotensin II-mediated vasoconstriction. The compound also inhibits oxidative stress and apoptosis via the PI3K/Akt signaling pathway. Its activity as an ACE inhibitor is well-characterized in biochemical assays. |
| ln Vivo |
Benazepril hydrochloride (3 or 10 mg/kg/d, p.o. for 14 days) dose-dependently inhibits the increase in the blood pressure caused by continuous norepinephrine (NE) infusion in spontaneously hypertensive rats (SHR) and suppresses in seizures induced by a monoamine oxidase inhibitor, tranylcypromine in NE infused SHR. Benazepril hydrochloride (30 mg/kg p.o.) decreases the triglyceride and total cholesterol levels in normotensive rats. Benazepril hydrochloride (3 mg/kg s.c.) causes a significant decrease in aortic atherosclerosis without reducing hypercholesterolemia in cholesterol-fed rabbits. Benazepril hydrochloride (100 mg/kg p.o.) shows no effect on the urine volume and urinary excretion of electrolytes but decreases PSP excretion in normotensive rats. Benazepril hydrochloride (10 mg/kg p.o.) inhibits the increase in the excretion of urinary protein in DOCA/salt spontaneously hypertensive rats. Benazepril Hydrochloride administration corrects systemic hypertension and significantly reduces angiotensin II and aldosterone in cats with experimentally induced or spontaneously occurring chronic renal failure. Benazepril hydrochloride administration reduces serum creatinine and urinary protein concentration in cat with experimentally induced or spontaneously occurring chronic renal failure. Benazepril hydrochloride significantly decreases blood pressure, angiotensin II and aldosterone and, increases upon discontinuation of administration to the pre-administration levels in a canine remnant kidney model of chronic renal failure. |
| Enzyme Assay |
Non-cellular enzyme assays for Benazepril HCl involve measuring its inhibition of ACE activity. These assays typically use purified ACE or tissue homogenates and a synthetic substrate, measuring the rate of substrate conversion to determine the compound's inhibitory potency. As a prodrug, its activity is often assessed after conversion to its active form, benazeprilat. Such assays are essential for characterizing its potency as an ACE inhibitor.
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| Cell Assay |
In vitro cell-based assays for Benazepril HCl are used to study its effects on cells. For example, studies have investigated its ability to inhibit oxidative stress and apoptosis through the PI3K/Akt signaling pathway. These experiments help to elucidate its mechanism of action beyond ACE inhibition, such as its protective effects on cells.
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| Animal Protocol |
Rats |
| ADME/Pharmacokinetics |
Benazepril HCl is an orally active compound. It is a prodrug that is metabolized to its active form, benazeprilat, in the liver. As an ACE inhibitor, it is well-absorbed and has a pharmacokinetic profile suitable for once- or twice-daily dosing. It is excreted primarily via the kidneys. Its half-life and other PK parameters are well-characterized.
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| Toxicity/Toxicokinetics |
Benazepril HCl has an established safety profile from its clinical use. It is generally well-tolerated, with side effects typical of ACE inhibitors, such as cough and hypotension. It is associated with a low rate of transient serum aminotransferase elevations and has been linked to rare instances of acute liver injury. Benazepril HCl is an approved drug for the treatment of hypertension.
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| References |
Arzneimittelforschung.1991 Jun;41(6):602-7;J Vet Med Sci.2007 Oct;69(10):1015-23.
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| Additional Infomation |
Benazepril hydrochloride is the hydrochloride salt formed by the reaction of benazepril with 1 molar equivalent of hydrogen chloride. It is used as a prodrug of the angiotensin-converting enzyme inhibitor benazepril to treat hypertension and heart failure. It is an EC 3.4.15.1 (peptidyl dipeptidase A) inhibitor. It contains the benazepril (1+) ion. Benazepril hydrochloride is the hydrochloride salt of benazepril, a carboxyl-containing angiotensin-converting enzyme (ACE) inhibitor with antihypertensive activity. As a prodrug, benazepril is metabolized to its active form, benazepril. Benazepril competitively binds to and inhibits ACE, thereby blocking the conversion of angiotensin I to angiotensin II. This inhibits the potent vasoconstrictive effect of angiotensin II, leading to vasodilation. Benazepril also reduces adrenal cortex aldosterone secretion for angiotensin II, thereby increasing sodium excretion and ultimately increasing water excretion. See also: Benazepril (containing active ingredient); Benazepril (containing active ingredient); Amlodipine besylate; Benazepril hydrochloride (ingredient)... See more...
Benazepril HCl (CGS14824A) is an orally active ACE inhibitor prodrug that is metabolized to its active form, benazeprilat. It is used to treat hypertension and has shown benefits in diabetic nephropathy. Benazepril HCl is an approved drug with a well-established clinical profile. |
| Molecular Formula |
C24H28N2O5.HCL
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| Molecular Weight |
460.95
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| Exact Mass |
460.176
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| CAS # |
86541-74-4
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| Related CAS # |
Benazepril;86541-75-5;Benazepril-d5 hydrochloride;1279026-26-4
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| PubChem CID |
5362123
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| Appearance |
White to off-white solid powder
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| Boiling Point |
691.2ºC at 760 mmHg
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| Melting Point |
188-190°C
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| Flash Point |
371.8ºC
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| LogP |
3.831
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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 |
10
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| Heavy Atom Count |
32
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| Complexity |
619
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| Defined Atom Stereocenter Count |
2
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| SMILES |
CCOC(=O)[C@H](CCC1=CC=CC=C1)N[C@H]2CCC3=CC=CC=C3N(C2=O)CC(=O)O.Cl
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| InChi Key |
VPSRQEHTHIMDQM-FKLPMGAJSA-N
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| InChi Code |
InChI=1S/C24H28N2O5.ClH/c1-2-31-24(30)20(14-12-17-8-4-3-5-9-17)25-19-15-13-18-10-6-7-11-21(18)26(23(19)29)16-22(27)28;/h3-11,19-20,25H,2,12-16H2,1H3,(H,27,28);1H/t19-,20-;/m0./s1
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| Chemical Name |
(3S)-3-[[(1S)-1-(Ethoxycarbonyl)-3-phenylpropyl]amino]-2,3,4,5-tetrahydro-2-oxo-1H-1-benzazepine-1-acetic acid hydrochloride
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| Synonyms |
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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: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.42 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 (5.42 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 (5.42 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 55 mg/mL (119.32 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1694 mL | 10.8472 mL | 21.6943 mL | |
| 5 mM | 0.4339 mL | 2.1694 mL | 4.3389 mL | |
| 10 mM | 0.2169 mL | 1.0847 mL | 2.1694 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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