| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
| Targets |
Angiotensin AT1 receptor[1].
Angiotensin AT1 receptor (with reduced activity compared to angiotensin II), AT2 receptor (selective binding, IC50=48.6 nM in HEK293 cells), and AT4 receptor (IC50=1.6 nM in bovine aortic endothelial cell membranes). |
|---|---|
| ln Vitro |
In HEK293 cells expressing rat receptors, it shows selective binding to AT2 over AT1 receptors (IC50s of 48.6 nM vs >1,000 nM). It induces a positive chronotropic effect in isolated rat right atria with an EC50 of 4.68 microM.
|
| ln Vivo |
Rats under anesthesia exhibit endothelium-dependent renal cortical vasodilatation upon exposure to human angiotensin II (3–8). Human Angiotensin II (3–8) has no cardiovascular effects at dosages up to 125 pmol/kg, but at 1.25 and 12.5 nmol/kg, there are dose-dependent increases in mean arterial blood pressure and decreases in renal and mesenteric flows as well as vascular conductances[1].
In anesthetized rats, it causes endothelium-dependent renal cortical vasodilation. At doses of 1.25 and 12.5 nmol/kg, it induces dose-dependent increases in mean arterial blood pressure and decreases in renal and mesenteric blood flows. At doses up to 125 pmol/kg, it shows no cardiovascular effects. |
| Enzyme Assay |
Competitive binding assays using radiolabeled angiotensin II or FITC-labeled ligands and membrane preparations from receptor-expressing cells (e.g., HEK293 expressing rat AT1/AT2) or rat liver. Membranes are incubated with the test compound and a fixed concentration of labeled ligand; bound radioactivity is measured after filtration.
|
| Cell Assay |
Vascular smooth muscle cells (VSMCs) are cultured and treated with the peptide. Cellular responses such as cAMP production, inositol phosphate accumulation, or calcium flux are measured. Alternatively, HEK293 cells overexpressing AT1 or AT2 receptors are used for receptor-specific signaling studies.
|
| Animal Protocol |
In anesthetized rats, the compound is administered intravenously at various doses (e.g., 125 pmol/kg, 1.25 nmol/kg, 12.5 nmol/kg). Hemodynamic parameters including mean arterial pressure, renal and mesenteric blood flows, and vascular conductances are continuously monitored.
|
| ADME/Pharmacokinetics |
Intravenously administered angiotensin peptides generally have a very short plasma half-life (less than one minute) due to rapid metabolism by aminopeptidases and angiotensin-converting enzyme 2 in plasma, erythrocytes, and major organs such as the kidney, liver, and lung.
|
| Toxicity/Toxicokinetics |
In animal studies, doses up to 125 pmol/kg produce no detectable cardiovascular effects. At higher doses of 1.25 and 12.5 nmol/kg, dose-dependent increases in mean arterial blood pressure and renal impairment are observed, indicating potential hypertensive and nephrotoxic effects at elevated concentrations.
|
| References | |
| Additional Infomation |
This hexapeptide (sequence: Val-Tyr-Ile-His-Pro-Phe) is a fragment of angiotensin II and is also known as angiotensin IV. It is less potent than full-length angiotensin II but shows higher selectivity for AT2 and AT4 receptors. It has been studied for potential cognitive-enhancing effects in animal models. Not approved for clinical use; strictly a research tool.
|
| Molecular Formula |
C42H55F3N8O10
|
|---|---|
| Molecular Weight |
888.93
|
| Related CAS # |
Angiotensin II (3-8), human;12676-15-2
|
| Sequence |
Val-Tyr-Ile-His-Pro-Phe
|
| Appearance |
Solid powder
|
| 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 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)
|
| Solubility (In Vitro) |
H2O :~50 mg/mL (~56.25 mM)
|
|---|---|
| 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 | 1.1249 mL | 5.6247 mL | 11.2495 mL | |
| 5 mM | 0.2250 mL | 1.1249 mL | 2.2499 mL | |
| 10 mM | 0.1125 mL | 0.5625 mL | 1.1249 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
