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Angiotensin III, human, mouse

Cat No.:V33113 Purity: ≥98%
Angiotensin III, human, mouse is a heptapeptide and an agonist of angiotensin type 2 receptor (AT2R).
Angiotensin III, human, mouse
Angiotensin III, human, mouse Chemical Structure CAS No.: 13602-53-4
Product category: New2
This product is for research use only, not for human use. We do not sell to patients.
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Product Description
Angiotensin III, human, mouse is a heptapeptide and an agonist of angiotensin type 2 receptor (AT2R). The IC50s for AT2R and AT1R are 0.648 nM and 21.1 nM respectively.
Angiotensin III (human, mouse) (CAS 13602-53-4) is a heptapeptide (Arg-Val-Tyr-Ile-His-Pro-Phe) that acts as an agonist of angiotensin receptors. It has a molecular formula of C₄₆H₆₆N₁₂O₉ and a molecular weight of 931.09. Angiotensin III is derived from the enzymatic cleavage of angiotensin II and plays a crucial role in the regulation of blood pressure and fluid balance. It is a preferred agonist for renal AT2 receptors, which are responsible for sodium excretion. The compound has IC₅₀ values of 0.648 nM for AT2R and 21.1 nM for AT1R.
Biological Activity I Assay Protocols (From Reference)
Targets
Angiotensin III targets angiotensin type 1 (AT1) and angiotensin type 2 (AT2) receptors. It has a 30-fold higher affinity for AT2 compared with AT1 in HEK293 cells. The IC₅₀ values for AT2R and AT1R are 0.648 nM and 21.1 nM, respectively. Angiotensin III is the preferred agonist for renal AT2 receptors, which are responsible for sodium excretion into the urine. The peptide plays a crucial role in the regulation of blood pressure and fluid balance.
ln Vitro
The heptapeptide angiotensin III (human, mouse) functions as an endogenous agonist of the angiotensin type 2 receptor (AT2R), with IC50 values for AT2R and AT1R of 0.648 nM and 21.1 nM, respectively [1].
In vitro, angiotensin III is a potent agonist at both AT1 and AT2 receptors. It has a 30-fold higher affinity for AT2 compared with AT1 in HEK293 cells. The IC₅₀ values for AT2R and AT1R are 0.648 nM and 21.1 nM, respectively. Angiotensin III stimulates aldosterone secretion and influences vasoconstriction. The peptide's activity is typically assessed by measuring receptor activation in cell-based assays.
ln Vivo
In SD rats, angiotensin III (7, 14 and 28 nmol/kg/min) increases fractional sodium excretion (FENa), fractional lithium excretion (FELi) and urine natriuresis (UNaV) [2]. Rats with elevated blood pressure are the result of angiotensin III's stimulation of sympathetic nerve activity, vasopressin production, and inhibition of baroreflex in the renin-angiotensin system [3].
In vivo, angiotensin III plays a crucial role in the regulation of blood pressure and fluid balance. It is derived from the enzymatic cleavage of angiotensin II and acts primarily on angiotensin receptors. Angiotensin III is the preferred agonist for renal AT2 receptors, which are responsible for sodium excretion. The peptide influences vasoconstriction and aldosterone secretion. However, specific in vivo efficacy studies have not been extensively reported.
Enzyme Assay
In vitro enzyme/receptor binding assays for angiotensin III typically involve competition binding studies using membranes from cells expressing human AT1 or AT2 receptors. The peptide is incubated with various concentrations of radiolabeled ligand (e.g., ¹²⁵I-angiotensin II) in binding buffer. Nonspecific binding is determined in the presence of excess unlabeled angiotensin II or a specific receptor antagonist. Following incubation, bound and free ligand are separated by filtration, and bound radioactivity is measured by gamma counting. IC₅₀ values are calculated by nonlinear regression analysis.
Cell Assay
In vitro cell-based assays for angiotensin III typically employ HEK293 cells or other cell lines stably expressing human AT1 or AT2 receptors. Cells are cultured in appropriate medium and treated with various concentrations of the peptide. Receptor activation is assessed by measuring intracellular calcium mobilization (for AT1) or other downstream signaling events (e.g., cAMP modulation for AT2). EC₅₀ values are determined from concentration-response curves. The peptide's activity is compared to that of angiotensin II.
Animal Protocol
In vivo animal studies with angiotensin III have not been extensively reported. The peptide is a component of the renin-angiotensin system and plays a role in blood pressure regulation. However, specific animal studies evaluating its pharmacokinetics or efficacy have not been described in the available literature. Angiotensin II and its analogs are more commonly studied in vivo.
ADME/Pharmacokinetics
Pharmacokinetic (PK) properties of angiotensin III have not been extensively characterized. As a peptide hormone, angiotensin III is rapidly metabolized by peptidases in the circulation and tissues. The compound has a short half-life in vivo, typically in the range of minutes. It is not orally bioavailable and requires parenteral administration for in vivo studies. Specific PK parameters have not been reported.
Toxicity/Toxicokinetics
The toxicity profile of angiotensin III has not been extensively characterized. As an endogenous peptide, angiotensin III is part of the normal physiological regulation of blood pressure. However, excessive activation of angiotensin receptors can lead to hypertension and cardiovascular pathology. The compound is intended for research use only and is not approved for therapeutic applications.
References

[1]. Relative affinity of angiotensin peptides and novel ligands at AT1 and AT2 receptors. Clin Sci (Lond). 2011 Oct;121(7):297-303.

[2]. Intrarenal angiotensin III is the predominant agonist for proximal tubule angiotensin type 2 receptors. Hypertension. 2012 Aug;60(2):387-95.

[3]. A new strategy for treating hypertension by blocking the activity of the brain renin-angiotensin system with aminopeptidase A inhibitors. Clin Sci (Lond). 2014 Aug;127(3):135-48.

Additional Infomation
Angiotensin III is a peptide. Angiotensin III is a heptapeptide formed by removing the N-terminal amino acid from angiotensin II via aminopeptidase A. Like angiotensin II, angiotensin III promotes aldosterone secretion and regulates renal blood flow, but its vasopressor activity is lower (approximately 40%).
Angiotensin III (human, mouse) is a research-grade heptapeptide agonist of angiotensin AT1 and AT2 receptors. It has a 30-fold higher affinity for AT2 compared with AT1 in HEK293 cells. IC₅₀ values: 0.648 nM for AT2R and 21.1 nM for AT1R. The peptide plays a role in blood pressure regulation, vasoconstriction, and aldosterone secretion. It is not an approved therapeutic drug. Molecular formula: C₄₆H₆₆N₁₂O₉; molecular weight: 931.09. Sequence: Arg-Val-Tyr-Ile-His-Pro-Phe. Synonyms include Angiotensin III and 2-8-angiotensin II.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C46H66N12O9
Molecular Weight
931.091240000001
Exact Mass
930.508
CAS #
13602-53-4
Related CAS #
Angiotensin III, human, mouse TFA
PubChem CID
3082042
Appearance
White to off-white solid powder
Density
1.39g/cm3
Index of Refraction
1.657
LogP
3.719
Hydrogen Bond Donor Count
11
Hydrogen Bond Acceptor Count
12
Rotatable Bond Count
25
Heavy Atom Count
67
Complexity
1680
Defined Atom Stereocenter Count
8
SMILES
CC[C@H](C)[C@@H](C(=O)N[C@@H](CC1=CN=CN1)C(=O)N2CCC[C@H]2C(=O)N[C@@H](CC3=CC=CC=C3)C(=O)O)NC(=O)[C@H](CC4=CC=C(C=C4)O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCN=C(N)N)N
InChi Key
QMMRCKSBBNJCMR-KMZPNFOHSA-N
InChi Code
InChI=1S/C46H66N12O9/c1-5-27(4)38(57-40(61)33(21-29-15-17-31(59)18-16-29)53-42(63)37(26(2)3)56-39(60)32(47)13-9-19-51-46(48)49)43(64)54-34(23-30-24-50-25-52-30)44(65)58-20-10-14-36(58)41(62)55-35(45(66)67)22-28-11-7-6-8-12-28/h6-8,11-12,15-18,24-27,32-38,59H,5,9-10,13-14,19-23,47H2,1-4H3,(H,50,52)(H,53,63)(H,54,64)(H,55,62)(H,56,60)(H,57,61)(H,66,67)(H4,48,49,51)/t27-,32-,33-,34-,35-,36-,37-,38-/m0/s1
Chemical Name
(2S)-2-[[(2S)-1-[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-5-(diaminomethylideneamino)pentanoyl]amino]-3-methylbutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]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

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 Data
Solubility (In Vitro)
H2O : ~100 mg/mL (~107.40 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 : PEG300Tween 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).
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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 : PEG300Tween 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).
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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 1.0740 mL 5.3701 mL 10.7401 mL
5 mM 0.2148 mL 1.0740 mL 2.1480 mL
10 mM 0.1074 mL 0.5370 mL 1.0740 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.

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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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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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