| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg | |||
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| 250mg | |||
| Other Sizes |
Purity: ≥98%
Benazeprilat (formerly known as CGS-14831), the active metabolite of the benazepril, is a potent inhibitor of angiotensin converting enzyme (ACE) with IC50 of 0.28 nM in plasma from dog.
| ln Vivo |
A good antihypertensive effect can be achieved by combining benazeprilat (10 mg/kg, intravenous injection) with amlodipine (0.5 mg/kg, intravenous injection) [2]. Oral benazepril (0.7 mg/kg) dramatically alters the kinetics of the systemic RAAS peptide, leading to a marked reduction in AII and ALD and an increase in PRA and AI [3].
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| Animal Protocol |
Animal/Disease Models: Male SHR (14-16 weeks old, 250-350 grams) [2].
Doses: 10 mg/kg Route of Administration: IV; one time/day for 2 days Experimental Results: A hypotensive effect occurs. Animal/Disease Models: Beagle dog (12.0-19.5 kg) [3]. Doses: 0.7 mg/kg Route of Administration: Orally, one time/day for 5 days. Experimental Results: Effects of systemic RAAS peptides. The tissue distribution of benazeprilat was assessed in rats. Following oral administration of its prodrug, benazepril, at doses ranging from 1 to 45 mg/kg, the animals were evaluated to determine the extent of ACE inhibition across different tissues [1]. |
| References |
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| Additional Infomation |
Benazeprilat is a benzodiazepine compound with the chemical name 1,3,4,5-tetrahydro-2H-1-benzodiazepine-2-one, in which the hydrogen atom bonded to the nitrogen atom is replaced by a carboxylmethyl group, and the 3-pro-S hydrogen is replaced by the amino group of (2S)-2-amino-4-phenylbutyric acid. It is an angiotensin-converting enzyme inhibitor, and its monoester prodrug, Benazeprilat, is used to treat hypertension and heart failure. It is an EC 3.4.15.1 (peptidyl dipeptidase A) inhibitor. It is a benzodiazepine compound belonging to the dicarboxylic acid and lactam class of compounds. Benazeprilat is an angiotensin-converting enzyme inhibitor. The mechanism of action of Benazeprilat is as an angiotensin-converting enzyme inhibitor. The physiological effect of Benazeprilat is achieved by lowering blood pressure. Benazeprilat is the active metabolite of Benazeprilat, a carboxyl-containing angiotensin-converting enzyme (ACE) inhibitor with antihypertensive effects. The prodrug Benazeprilat is metabolized in the liver to Benazeprilat, which competitively binds to and inhibits ACE, thereby blocking the conversion of angiotensin I to angiotensin II. This prevents the potent vasoconstrictive effect of angiotensin II, leading to vasodilation. Benazeprilat also reduces adrenal cortex aldosterone secretion for angiotensin II, thereby increasing sodium excretion and consequently increasing water excretion.
See also: Benazeprilat hydrochloride (active ingredient). |
| Molecular Formula |
C22H24N2O5
|
|---|---|
| Molecular Weight |
396.443
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| Exact Mass |
396.169
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| CAS # |
86541-78-8
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| Related CAS # |
Benazeprilat-d5;1279033-05-4
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| PubChem CID |
5463984
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| Appearance |
White to off-white solid powder
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| Density |
1.34 g/cm3
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| Boiling Point |
711.3ºC at 760 mmHg
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| Melting Point |
270-272ºC
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| Flash Point |
384ºC
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| Index of Refraction |
1.643
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| LogP |
2.55
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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 |
8
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| Heavy Atom Count |
29
|
| Complexity |
590
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| Defined Atom Stereocenter Count |
2
|
| SMILES |
C(N1C(=O)[C@@H](N[C@H](C(=O)O)CCC2C=CC=CC=2)CCC2C=CC=CC1=2)C(=O)O
|
| InChi Key |
MADRIHWFJGRSBP-ROUUACIJSA-N
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| InChi Code |
InChI=1S/C22H24N2O5/c25-20(26)14-24-19-9-5-4-8-16(19)11-13-17(21(24)27)23-18(22(28)29)12-10-15-6-2-1-3-7-15/h1-9,17-18,23H,10-14H2,(H,25,26)(H,28,29)/t17-,18-/m0/s1
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| Chemical Name |
(2S)-2-[[(3S)-1-(carboxymethyl)-2-oxo-4,5-dihydro-3H-1-benzazepin-3-yl]amino]-4-phenylbutanoic acid
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| Synonyms |
Benazeprilat CGS 14831 CGS-14831 CGS14831
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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 | 2.5224 mL | 12.6122 mL | 25.2245 mL | |
| 5 mM | 0.5045 mL | 2.5224 mL | 5.0449 mL | |
| 10 mM | 0.2522 mL | 1.2612 mL | 2.5224 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00835367 | COMPLETEDWITH RESULTS | Drug: Amlodipine-benazepril 10 mg-20 mg capsules Drug: Lotrel® 10 mg-20 mg capsule |
Healthy | Teva Pharmaceuticals USA | 2004-03 | Phase 1 |
| NCT00836576 | COMPLETED | Drug: Benazepril HCl 40 mg Tablets Drug: Lotensin® 40 mg Tablets |
Healthy | Teva Pharmaceuticals USA | 2001-02 | Phase 1 |
| NCT00836537 | COMPLETED | Drug: Benazepril HCl 40 mg Tablets Drug: Lotensin® 40 mg Tablets |
Healthy | Teva Pharmaceuticals USA | 2001-03 | Phase 1 |
| NCT00834977 | COMPLETEDWITH RESULTS | Drug: Amlodipine-benazepril 10 mg-20 mg capsules Drug: Lotrel® 10 mg-20 mg capsule |
Healthy | Teva Pharmaceuticals USA | 2004-04 | Phase 1 |
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