| Size | Price | Stock | Qty |
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| ln Vivo |
For oral angiotensin-converting enzyme (ACE) inhibition in rats and dogs as well as for antihypertensive efficacy in rats, captopril and pivalopril, a novel molecule with a hindered sulfur group, have been evaluated. In various groups of conscious normotensive rats, rivacapril (0.03-1.0 mg/kg, orally [po]) demonstrated dose-related inhibition of angiotensin I (AngI)-induced pressor effects. Both captopril and rivastigmine have an ED50 of 0.1 mg/kg. Pivalopril causes a dose-related antagonistic impact on the pressor effects of AngI in conscious, normotensive dogs when administered orally in increments of 0.01–1.0 mg/kg. Pitavapril's ED50 is 0.17 mg/kg, while captopril's ED50 is 0.06 mg/kg. Both chemicals act for about the same amount of time at identical doses. In sodium-deficient, consciously hypertensive rats (SHR), rivalevopril (1–100 mg/kg, po) reduces mean arterial pressure in a dose-related manner. Similar to captopril in terms of potency and longevity. When given orally for five days, pivalopril (100 mg/kg daily) was found to be more effective in lowering mean arterial pressure in sodium-repleted SHR patients than captopril (100 mg/kg daily). It was determined that pivalopril is an effective ACE inhibitor and antihypertensive medication that may be used orally [2].
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| References | |
| Additional Infomation |
Pivopril is a N-acyl-amino acid.
Pivopril is an angiotensin-converting enzyme (ACE) inhibitor with antihypertensive activity. Upon hydrolysis, the free SH metabolite of pivopril competitively binds to and inhibits ACE, thereby blocking the conversion of angiotensin I to angiotensin II. This prevents the potent vasoconstrictive actions of angiotensin II and results in vasodilation. Pivopril also decreases angiotensin II-induced aldosterone secretion by the adrenal cortex, which leads to an increase in sodium excretion and subsequently increases water outflow. |
| Molecular Formula |
C16H27NO4S
|
|---|---|
| Molecular Weight |
329.454883813858
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| Exact Mass |
329.166
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| CAS # |
81045-50-3
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| PubChem CID |
6917956
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| Appearance |
White to off-white solid powder
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| Density |
1.16g/cm3
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| Boiling Point |
490.431°C at 760 mmHg
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| Flash Point |
250.4±26.8 °C
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| Vapour Pressure |
0.0±2.7 mmHg at 25°C
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| Index of Refraction |
1.531
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| LogP |
2.784
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
22
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| Complexity |
424
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C[C@H](CSC(=O)C(C)(C)C)C(=O)N(CC(=O)O)C1CCCC1
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| InChi Key |
XRKXJJYSKUIIEN-LLVKDONJSA-N
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| InChi Code |
InChI=1S/C16H27NO4S/c1-11(10-22-15(21)16(2,3)4)14(20)17(9-13(18)19)12-7-5-6-8-12/h11-12H,5-10H2,1-4H3,(H,18,19)/t11-/m1/s1
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| Chemical Name |
2-[cyclopentyl-[(2S)-3-(2,2-dimethylpropanoylsulfanyl)-2-methylpropanoyl]amino]acetic 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 |
| 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 : ~90 mg/mL (~273.18 mM)
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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 | 3.0354 mL | 15.1768 mL | 30.3536 mL | |
| 5 mM | 0.6071 mL | 3.0354 mL | 6.0707 mL | |
| 10 mM | 0.3035 mL | 1.5177 mL | 3.0354 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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