Benazepril HCl (CGS14824A)

Alias: CGS 14824A HCl; CGS14824A; Briem; CGS-14824-A;CGS-14824A;CGS-14824 A; Cibacène; Cibacen; Labopal; Lotensin
Cat No.:V1787 Purity: ≥98%
Benazepril HCl (formerly CGS 14824A;CGS-14824-A;Briem; Cibacène; Cibacen; Labopal; Lotensin), the hydrochloride salt of Benazepril which is a prodrug that can bemetabolized to its active formbenazeprilat,is a potent angiotensin I converting enzyme (ACE) inhibitor that has beenwidelyused primarily in treatment of hypertension.
Benazepril HCl (CGS14824A) Chemical Structure CAS No.: 86541-74-4
Product category: RAAS
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
250mg
500mg
1g
2g
10g
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Other Forms of Benazepril HCl (CGS14824A):

  • Benazepril (CGS 14824A)
  • Benazepril-d5 HCl
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Benazepril HCl (formerly CGS 14824A; CGS-14824-A; Briem; Cibacène; Cibacen; Labopal; Lotensin), the hydrochloride salt of Benazepril which is a prodrug that can be metabolized to its active form benazeprilat, is a potent angiotensin I converting enzyme (ACE) inhibitor that has been widely used primarily in treatment of hypertension. The mechanism of action of thie drug is to prevent the catalytic conversion of angiotensin I to angiotensin II and in turn causes vasodilation and an increase in capillary blood volume. Benazepril hydrochloride dose-dependently inhibits the increase in the blood pressure caused by continuous norepinephrine infusion in spontaneously hypertensive rats and suppresses in seizures.

Biological Activity I Assay Protocols (From Reference)
ln Vitro

In vitro activity: 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.

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.
Animal Protocol
3 or 10 mg/kg/d, p.o. for 14 days
Rats
References
Arzneimittelforschung.1991 Jun;41(6):602-7;J Vet Med Sci.2007 Oct;69(10):1015-23.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C24H28N2O5.HCL
Molecular Weight
460.95
CAS #
86541-74-4
Related CAS #
Benazepril;86541-75-5;Benazepril-d5 hydrochloride;1279026-26-4
SMILES
Cl[H].O=C1[C@]([H])(C([H])([H])C([H])([H])C2=C([H])C([H])=C([H])C([H])=C2N1C([H])([H])C(=O)O[H])N([H])[C@]([H])(C(=O)OC([H])([H])C([H])([H])[H])C([H])([H])C([H])([H])C1C([H])=C([H])C([H])=C([H])C=1[H]
InChi Key
VPSRQEHTHIMDQM-FKLPMGAJSA-N
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
Chemical Name
(3S)-3-[[(1S)-1-(Ethoxycarbonyl)-3-phenylpropyl]amino]-2,3,4,5-tetrahydro-2-oxo-1H-1-benzazepine-1-acetic acid hydrochloride
Synonyms
CGS 14824A HCl; CGS14824A; Briem; CGS-14824-A;CGS-14824A;CGS-14824 A; Cibacène; Cibacen; Labopal; Lotensin
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)
Solubility Data
Solubility (In Vitro)
DMSO:92 mg/mL (199.6 mM)
Water:19 mg/mL (41.2 mM)
Ethanol:92 mg/mL (199.6 mM)
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.

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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.
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 corn oil and mix evenly.


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.

 (Please use freshly prepared in vivo formulations for optimal results.)
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.

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What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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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