| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
IC50: 9 μM (ACE)[1].
Angiotensin I-converting enzyme (ACE) is a key enzyme in the renin-angiotensin system that converts angiotensin I to the potent vasoconstrictor angiotensin II. H-Val-Pro-Pro-OH TFA inhibits ACE with an IC50 of 9 μM. By inhibiting ACE, the compound reduces the production of angiotensin II, leading to vasodilation and decreased blood pressure. The compound acts as an ACE inhibitor (antagonist). |
|---|---|
| ln Vitro |
Angiotensin I converting enzyme (ACE) may be inhibited by H-Val-Pro-Pro-OH (TFA), a derivative of proline peptides, with an IC50 of 9 μM[1]. In 3T3-F442A pre-adipocytes, H-Val-Pro-Pro-OH (TFA) may improve insulin sensitivity and avoid insulin resistance. Additionally, H-Val-Pro-Pro-OH (TFA) has anti-inflammatory and anti-hypertensive properties. H-Val-Pro-Pro-OH (TFA)) improves adipocytes' expression of the glucose transporter 4 (GLUT4) and helps TNF-treated adipocytes' ability to absorb glucose[2].
In vitro, H-Val-Pro-Pro-OH TFA inhibits ACE with an IC50 of 9 μM. It acts as an ACE inhibitor. In cellular models, the compound has shown effects on 3T3-F442A pre-adipocytes, indicating potential effects on adipocyte differentiation and metabolism. The compound inhibits Angiotensin I converting enzyme with an IC50 of 9 μM. |
| ln Vivo |
In vivo, H-Val-Pro-Pro-OH TFA may be used to study the effects of ACE inhibition on blood pressure and cardiovascular function. It has shown effects in cellular models, including 3T3-F442A pre-adipocytes. By inhibiting ACE, the compound may have antihypertensive effects in animal models.
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| Enzyme Assay |
The in vitro enzyme activity assay for H-Val-Pro-Pro-OH TFA uses purified ACE and a fluorogenic or chromogenic substrate to measure the inhibitory activity of the compound. The IC50 is determined from dose-response curves. The compound is incubated with ACE and substrate, and the rate of substrate cleavage is measured to determine the degree of inhibition.
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| Cell Assay |
Cell-based assays using ACE-expressing cells or relevant cell lines (e.g., 3T3-F442A pre-adipocytes) are performed to evaluate the cellular effects of ACE inhibition by H-Val-Pro-Pro-OH TFA. Cells are treated with the compound, and downstream effects on angiotensin II production, cell proliferation, or differentiation are measured.
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| Animal Protocol |
In vivo studies using animal models of hypertension are performed to evaluate the effects of H-Val-Pro-Pro-OH TFA on blood pressure and cardiovascular function. The compound is administered via various routes, and blood pressure is measured using telemetry or tail-cuff methods. The antihypertensive effects of the compound are assessed relative to vehicle controls.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for H-Val-Pro-Pro-OH TFA are limited. As a peptide derivative, it may have limited oral bioavailability and is typically used in research applications. The compound is a tripeptide with a TFA salt, which may affect its stability and absorption. Further pharmacokinetic studies are needed to fully characterize the ADME properties of this compound.
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| Toxicity/Toxicokinetics |
Preclinical toxicology data for H-Val-Pro-Pro-OH TFA are limited. The compound is used for research purposes only. No significant toxicities have been reported in the literature. Further toxicological evaluation is needed to assess the safety of the compound for potential therapeutic applications.
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| References |
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| Additional Infomation |
H-Val-Pro-Pro-OH TFA (CAS: 2828433-08-3) is a research compound used to study ACE inhibition and the role of the renin-angiotensin system in physiology and disease. The compound is a milk-derived proline peptide derivative. H-Val-Pro-Pro-OH TFA is not approved for human use and is intended for research purposes only. The compound is a valuable tool for investigating the physiological and pathological roles of ACE and the renin-angiotensin system.
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| Molecular Formula |
C17H26F3N3O6
|
|---|---|
| Molecular Weight |
425.400055408478
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| Exact Mass |
425.177
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| CAS # |
2828433-08-3
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| Related CAS # |
H-Val-Pro-Pro-OH;58872-39-2
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| PubChem CID |
137319716
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| Appearance |
White to off-white solid powder
|
| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
29
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| Complexity |
549
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| Defined Atom Stereocenter Count |
3
|
| SMILES |
C(F)(F)(F)C(=O)O.C(N1CCC[C@H]1C(=O)O)([C@@H]1CCCN1C(=O)[C@@H](N)C(C)C)=O
|
| InChi Key |
DJQRQUZDHQFFTH-LFELFHSZSA-N
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| InChi Code |
InChI=1S/C15H25N3O4.C2HF3O2/c1-9(2)12(16)14(20)17-7-3-5-10(17)13(19)18-8-4-6-11(18)15(21)22;3-2(4,5)1(6)7/h9-12H,3-8,16H2,1-2H3,(H,21,22);(H,6,7)/t10-,11-,12-;/m0./s1
|
| Chemical Name |
(2S)-1-[(2S)-1-[(2S)-2-amino-3-methylbutanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carboxylic acid;2,2,2-trifluoroacetic 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 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) |
H2O: 125 mg/mL (293.84 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 25 mg/mL (58.77 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3507 mL | 11.7536 mL | 23.5073 mL | |
| 5 mM | 0.4701 mL | 2.3507 mL | 4.7015 mL | |
| 10 mM | 0.2351 mL | 1.1754 mL | 2.3507 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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