Angiotensin II human (Angiotensin II) TFA is a vasoconstrictor and the major biologically active peptide of the renin/angiotensin system. Angiotensin II human TFA plays a central role in regulating human blood pressure, mainly through angiotensin II and G protein-coupled receptors (GPCRs), angiotensin II type 1 receptor (AT1R) and angiotensin II type 2 receptor. mediated by interactions between AT2Rs. Angiotensin II human TFA stimulates sympathetic stimulation, increases aldosterone biosynthesis and renal activity. Angiotensin II human TFA induces the growth of vascular smooth muscle cells and increases the synthesis of type I and type III collagen in fibroblasts, leading to thickening of blood vessel walls and myocardium, and leading to fibrosis. Angiotensin II human TFA also causes apoptosis. Angiotensin II human TFA induces endothelial cell capillary formation through a LOX-1-dependent redox-sensitive pathway.

Physicochemical Properties

Molecular Formula	C52H72F3N13O14
Molecular Weight	1160.20200252533
Exact Mass	1159.527
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
PubChem CID	146047991
Appearance	White to off-white solid powder
Hydrogen Bond Donor Count	14
Hydrogen Bond Acceptor Count	20
Rotatable Bond Count	29
Heavy Atom Count	82
Complexity	2060
Defined Atom Stereocenter Count	9
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
InChi Key	FYMJZKAYBCZPKL-PIONDTTLSA-N
InChi Code	InChI=1S/C50H71N13O12.C2HF3O2/c1-5-28(4)41(47(72)59-36(23-31-25-54-26-56-31)48(73)63-20-10-14-38(63)45(70)60-37(49(74)75)22-29-11-7-6-8-12-29)62-44(69)35(21-30-15-17-32(64)18-16-30)58-46(71)40(27(2)3)61-43(68)34(13-9-19-55-50(52)53)57-42(67)33(51)24-39(65)66;3-2(4,5)1(6)7/h6-8,11-12,15-18,25-28,33-38,40-41,64H,5,9-10,13-14,19-24,51H2,1-4H3,(H,54,56)(H,57,67)(H,58,71)(H,59,72)(H,60,70)(H,61,68)(H,62,69)(H,65,66)(H,74,75)(H4,52,53,55);(H,6,7)/t28-,33-,34-,35-,36-,37-,38-,40-,41-;/m0./s1
Chemical Name	(3S)-3-amino-4-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[(2S)-2-[[(1S)-1-carboxy-2-phenylethyl]carbamoyl]pyrrolidin-1-yl]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-oxobutanoic acid;2,2,2-trifluoroacetic 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 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)

Biological Activity

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]. International union of pharmacology. XXIII. The angiotensin II receptors. Pharmacol Rev. 2000 Sep;52(3):415-72. [2]. 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]. Angiotensin II induces capillary formation from endothelial cells via the LOX-1 dependent redox-sensitive pathway. Hypertension. 2007;50(5):952-957. [4]. Angiotensin II induces neutrophil accumulation in vivo through generation and release of CXC chemokines. Circulation. 2004;110(23):3581-3586. [5]. 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.

Solubility Data

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 (e.g. IP/IV/IM/SC) Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline) *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). 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)] *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. Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline) Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline) Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline) Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil) Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL 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). Oral Formulation 3: Dissolved in PEG400 Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose Oral Formulation 6: Mixing with food powders Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.  (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.