Size | Price | Stock | Qty |
---|---|---|---|
5mg |
|
||
10mg |
|
||
50mg |
|
||
Other Sizes |
|
Targets |
AT1 Receptor AT2 Receptor
|
---|---|
ln Vitro |
Angiotensin II human (Ang II) is recognized to have most of its actions through AT1 receptors, whereas AT2 receptors assist in controlling blood pressure and renal function [1]. Human angiotensin II elevates blood pressure (BP) by a number of mechanisms, the most significant of which are renal effects, sympathetic activation, vasoconstriction, and enhanced aldosterone production. Other human effects of angiotensin II include promotion of growth, cell migration, and mitosis in vascular smooth muscle cells, increased production of type I and type III collagen in fibroblasts, leading to thickening of vessel walls and myocardium, and fibrosis. Ang II receptor type 1 (AT1) mediates these actions [2]. Angiotensin II (1 nM) TFA promotes capillary development in human coronary artery endothelial cells and increases the production of LOX-1 and VEGF in the Matrigel assay. Apocynin, a glycolate phosphate oxidase inhibitor, and losartan, an Ang II type 1 receptor blocker, all inhibit angiotensin II-mediated VEGF and LOX-1 expression, capillary formation, intracellular reactive oxygen species production, and phosphorylation of p38 and p44/42 mitogen-activated protein kinase dinuclear [3]. The Ang II type 2 receptor blocker PD123319 is not inhibited by the anti-LOX-1 antibody nicotinamide adenine.
|
ln Vivo |
Angiotensin II human TFA (5 mL 1 nM; intraperitoneal injection; 200-250 g Sprague-Dawley rats) causes a considerable increase in neutrophil recruitment, which peaks at 4 hours and peaks at 24 hours [4]. An osmotic minipump was subcutaneously inserted into each rat to infuse Angiotensin II human TFA (1000 ng/kg/min) for four weeks in order to distinguish AT1 receptor populations that are essential for the etiology of hypertension. Angiotensin II human TFA activates AT1 receptors in the kidney, which increases salt reabsorption and results in hypertension [5].
|
References |
[1]. de Gasparo M, et al. International union of pharmacology. XXIII. The angiotensin II receptors. Pharmacol Rev. 2000 Sep;52(3):415-72.
[2]. Fyhrquist F, et al. Role of angiotensin II in blood pressure regulation and in the pathophysiology of cardiovascular disorders. J Hum Hypertens. 1995 Nov;9 Suppl 5:S19-24. [3]. Hu C, et al. Angiotensin II induces capillary formation from endothelial cells via the LOX-1 dependent redox-sensitive pathway. Hypertension. 2007;50(5):952-957. [4]. Nabah YN, et al. Angiotensin II induces neutrophil accumulation in vivo through generation and release of CXC chemokines. Circulation. 2004;110(23):3581-3586. [5]. Crowley SD, et al. Angiotensin II causes hypertension and cardiac hypertrophy through its receptors in the kidney. Proc Natl Acad Sci U S A. 2006 Nov 21;103(47):17985-90. |
Molecular Formula |
C52H72F3N13O14
|
---|---|
Molecular Weight |
1160.20
|
CAS # |
2761969-44-0
|
Related CAS # |
Angiotensin II human;4474-91-3;Angiotensin II human acetate;68521-88-0;Angiotensin II human-13C6,15N TFA
|
Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
|
SMILES |
C(F)(F)(F)C(=O)O.C(N1CCC[C@H]1C(=O)N[C@H](C(=O)O)CC1C=CC=CC=1)(=O)[C@@H](NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@@H](NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@@H](N)CC(=O)O)CC1C=CC(O)=CC=1)CC1NC=NC=1
|
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 (e.g. under nitrogen), avoid exposure to moisture and light. |
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 : 10 mg/mL (8.62 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 | 0.8619 mL | 4.3096 mL | 8.6192 mL | |
5 mM | 0.1724 mL | 0.8619 mL | 1.7238 mL | |
10 mM | 0.0862 mL | 0.4310 mL | 0.8619 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.