| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
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Delapril HCl is a novel and potent inhibitor of ACE (angiotensin-converting enzyme) with the potential to be used for the treatment of cardiovascular diseases.
| ln Vivo |
In spontaneously hypertensive rats (SHR), delapril (3 mg/kg; oral administration for 2 weeks) exhibits strong ACE inhibitory activity [1]. In several experimental models of hypertension, dilapril (1–10 mg/kg; oral) significantly and persistently lowers blood pressure [1].
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|---|---|
| Animal Protocol |
Animal/Disease Models: SHR[1]
Doses: 3 mg/kg Route of Administration: po (po (oral gavage)) 2 weeks Experimental Results: Effective ACE inhibitory activity. Animal/Disease Models: 2 kidneys, 1 hypertensive rat, dog and SHR[1] Doses: 1-10 mg/kg Route of Administration: Oral Experimental Results:It has significant and lasting antihypertensive effect. |
| References | |
| Additional Infomation |
Delapril hydrochloride is a peptide.
Delapril Hydrochloride is the hydrochloride salt of delapril, a lipophilic, non-sulfhydryl angiotensin-converting enzyme (ACE) inhibitor with antihypertensive activity. As a prodrug, delapril is converted to two active metabolites, delapril diacid and 5-hydroxy delapril diacid, which competitively bind to and inhibit ACE, thereby blocking the conversion of angiotensin I to angiotensin II. This prevents the potent vasoconstrictive actions of angiotensin II and results in vasodilation. Delapril also decreases angiotensin II-induced aldosterone secretion by the adrenal cortex, which leads to an increase in sodium excretion and subsequently increases water outflow. See also: Delapril (annotation moved to). |
| Molecular Formula |
C26H32N2O5CLH
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|---|---|
| Molecular Weight |
489.009
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| Exact Mass |
488.207
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| CAS # |
83435-67-0
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| Related CAS # |
Delapril-d3 hydrochloride;2714473-25-1;Delapril;83435-66-9
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| PubChem CID |
5362115
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| Appearance |
White to off-white solid powder
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| Boiling Point |
659.7ºC at 760 mmHg
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| Melting Point |
169ºC
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| Flash Point |
352.7ºC
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| LogP |
3.802
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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 |
12
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| Heavy Atom Count |
34
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| Complexity |
649
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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](C)C(=O)N(CC(=O)O)C2CC3=CC=CC=C3C2.Cl
|
| InChi Key |
FDJCVHVKXFIEPJ-JCNFZFLDSA-N
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| InChi Code |
InChI=1S/C26H32N2O5.ClH/c1-3-33-26(32)23(14-13-19-9-5-4-6-10-19)27-18(2)25(31)28(17-24(29)30)22-15-20-11-7-8-12-21(20)16-22;/h4-12,18,22-23,27H,3,13-17H2,1-2H3,(H,29,30);1H/t18-,23-;/m0./s1
|
| Chemical Name |
2-[2,3-dihydro-1H-inden-2-yl-[(2S)-2-[[(2S)-1-ethoxy-1-oxo-4-phenylbutan-2-yl]amino]propanoyl]amino]acetic acid;hydrochloride
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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. |
| 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 : ~250 mg/mL (~511.25 mM)
H2O : ~1.72 mg/mL (~3.52 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.25 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 20.8 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: ≥ 2.08 mg/mL (4.25 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 20.8 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: ≥ 2.08 mg/mL (4.25 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 | 2.0449 mL | 10.2247 mL | 20.4495 mL | |
| 5 mM | 0.4090 mL | 2.0449 mL | 4.0899 mL | |
| 10 mM | 0.2045 mL | 1.0225 mL | 2.0449 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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