| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 100mg |
|
||
| 250mg | |||
| 500mg | |||
| Other Sizes |
| ln Vivo |
The long-term and sustained antihypertensive effects of alapril in renally hypertensive rats were confirmed by continuous once-daily oral administration (1-2 mg/kg/d). Alapril (3 mg/kg) exhibits a stable and prolonged hypotensive effect in dogs with renal hypertension, with a longer half-life than captopril [1].
|
|---|---|
| References | |
| Additional Infomation |
Alexyl is a thioacetate dipeptide, belonging to EC 3.4.15.1 (peptidyl dipeptidase A) inhibitors. Alexyl is a long-acting, thiol-containing angiotensin-converting enzyme (ACE) inhibitor with antihypertensive effects. As a prodrug, alepril is rapidly metabolized to captopril; captopril competitively binds to and inhibits ACE activity, thereby blocking the conversion of angiotensin I to angiotensin II. This inhibits the potent vasoconstrictive effect of angiotensin II, leading to vasodilation. Captopril also reduces adrenal cortex aldosterone secretion for angiotensin II, thereby increasing sodium excretion and consequently increasing water excretion.
|
| Molecular Formula |
C20H26N2O5S
|
|---|---|
| Molecular Weight |
406.5
|
| Exact Mass |
406.156
|
| CAS # |
74258-86-9
|
| Related CAS # |
Alacepril; 74258-86-9
|
| PubChem CID |
71992
|
| Appearance |
White to off-white solid powder
|
| Density |
1.281g/cm3
|
| Boiling Point |
679.1ºC at 760 mmHg
|
| Flash Point |
364.5ºC
|
| Index of Refraction |
1.581
|
| LogP |
2.034
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
9
|
| Heavy Atom Count |
28
|
| Complexity |
591
|
| Defined Atom Stereocenter Count |
3
|
| SMILES |
C[C@H](CSC(=O)C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC2=CC=CC=C2)C(=O)O
|
| InChi Key |
FHHHOYXPRDYHEZ-COXVUDFISA-N
|
| InChi Code |
InChI=1S/C20H26N2O5S/c1-13(12-28-14(2)23)19(25)22-10-6-9-17(22)18(24)21-16(20(26)27)11-15-7-4-3-5-8-15/h3-5,7-8,13,16-17H,6,9-12H2,1-2H3,(H,21,24)(H,26,27)/t13-,16+,17+/m1/s1
|
| Chemical Name |
(2S)-2-[[(2S)-1-[(2S)-3-acetylsulfanyl-2-methylpropanoyl]pyrrolidine-2-carbonyl]amino]-3-phenylpropanoic acid
|
| HS Tariff Code |
2934.99.9001
|
| 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 (In Vitro) |
DMSO: ~100 mg/mL (~246.0 mM; with ultrasonication)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (6.15 mM) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and 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 (6.15 mM) 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; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. 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. Solubility in Formulation 3: 2.5 mg/mL (6.15 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4600 mL | 12.3001 mL | 24.6002 mL | |
| 5 mM | 0.4920 mL | 2.4600 mL | 4.9200 mL | |
| 10 mM | 0.2460 mL | 1.2300 mL | 2.4600 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
