| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| 1g | |||
| Other Sizes |
| Targets |
The target of Angiotensin II includes Angiotensin II type 1 receptor (AT1R) and Angiotensin II type 2 receptor (AT2R) [2][3]
Angiotensin I acts as a substrate for Angiotensin-converting enzyme (ACE) [1] |
|---|---|
| ln Vitro |
1. Conversion of Angiotensin I to Angiotensin II by ACE (Reference [1]): Incubation of Angiotensin I (0.1-1 μM, purified from human plasma) with ACE (isolated from rabbit lung) in Tris-HCl buffer (pH 7.4, 37°C) resulted in conversion to Angiotensin II. The reaction was quantified by measuring the pressor activity of the product in isolated rat aorta rings: Angiotensin I (0.5 μM) was completely converted to Angiotensin II within 10 minutes, with the product inducing a 2.5-fold increase in aortic contraction compared to the control [1]
2. Receptor binding of Angiotensin II (Reference [3]): Angiotensin II (1-100 nM) bound to AT1R-expressing CHO cells in a dose-dependent manner. Scatchard analysis showed a dissociation constant (Kd) of 0.8 nM for AT1R, with a maximum binding capacity (Bmax) of 500 fmol/mg protein [3] |
| ln Vivo |
1. Pressor effect of Angiotensin I and Angiotensin II in anesthetized dogs (Reference [1]): Intravenous injection of Angiotensin I (1 μg/kg) caused a gradual increase in mean arterial pressure (MAP) from 90 mmHg to 135 mmHg within 2 minutes, which persisted for 5 minutes. Injection of Angiotensin II (0.5 μg/kg) induced a more rapid pressor response (MAP peaked at 140 mmHg within 30 seconds) and shorter duration (2 minutes). Pretreatment with ACE inhibitor (captopril, 10 mg/kg) abolished the pressor effect of Angiotensin I but not Angiotensin II [1]
2. Vasoconstrictive effect in rabbits (Reference [1]): Intracoronary infusion of Angiotensin II (0.1 μg/min) reduced coronary blood flow by 40% in anesthetized rabbits, while Angiotensin I (0.2 μg/min) caused a 30% reduction (blocked by captopril) [1] |
| Enzyme Assay |
1. ACE-catalyzed conversion assay of Angiotensin I (Reference [1]): Prepare a reaction mixture containing Angiotensin I (0.5 μM), ACE (10 mU/mL, rabbit lung), and Tris-HCl buffer (50 mM, pH 7.4, containing 100 mM NaCl). Incubate the mixture at 37°C for 0-20 minutes. Terminate the reaction by adding trichloroacetic acid (10% w/v). The amount of Angiotensin II formed was determined by measuring the pressor activity in isolated rat aorta (precontracted with norepinephrine, 1 μM) — the contraction amplitude of the aorta was calibrated against a standard curve of Angiotensin II (0.1-1 μM) [1]
|
| ADME/Pharmacokinetics |
1. Metabolism of angiotensin I (References [1][2]): Angiotensin I has a plasma half-life of approximately 1 minute in the human body and is mainly metabolized by angiotensin-converting enzyme (ACE) in the lungs and vascular endothelial cells to generate angiotensin II. A small amount (10%) of angiotensin I is degraded into inactive fragments (e.g., angiotensin 1-7) by neutral endopeptidases [1][2]. 2. Pharmacokinetics of angiotensin II (Reference [3]): Angiotensin II has a plasma half-life of approximately 15 seconds in the human body and is rapidly cleared in the kidneys and liver by angiotensinases (e.g., aminopeptidase A, carboxypeptidase N). It cannot cross the blood-brain barrier and is not orally absorbed (bioavailability <1%) [3].
|
| Toxicity/Toxicokinetics |
1. Acute cardiovascular effects of angiotensin II (References [1][3]): Overdose of angiotensin II (5 μg/kg in dogs) can lead to severe hypertension (mean arterial pressure >180 mmHg), ventricular arrhythmias, and myocardial ischemia [1][3]
2. Plasma protein binding rate (References [2][3]): Angiotensin I and angiotensin II have low plasma protein binding rates in humans (15-20% and 10-15%, respectively), and are mainly bound to albumin [2][3] |
| References | |
| Additional Infomation |
1. Sources and physiological functions (References [1][2][3]): Angiotensin I is a decapeptide (Asp-Arg-Val-Tyr-Ile-His-Pro-Phe-His-Leu) synthesized from angiotensinogen (liver-derived) via renin (kidney-derived) cleavage. Angiotensin II is an octapeptide (Asp-Arg-Val-Tyr-Ile-His-Pro-Phe) formed by the removal of the angiotensin I-terminal dipeptide (His-Leu) mediated by angiotensin-converting enzyme (ACE). Both are key components of the renin-angiotensin system (RAS), regulating blood pressure, fluid balance, and vascular tone [1][2][3]
2. Clinical significance (References [1][3]): Angiotensin II dysregulation (excessive production or enhanced AT1R activity) is associated with hypertension, heart failure, and kidney disease. ACE inhibitors and AT1R blockers (ARBs) are used clinically to inhibit angiotensin II-mediated effects [1][3] |
| Molecular Formula |
C30H48N8O9
|
|---|---|
| Molecular Weight |
664.75000
|
| Exact Mass |
664.354
|
| CAS # |
58442-64-1
|
| Related CAS # |
Angiotensin I/II (1-5) (TFA)
|
| PubChem CID |
9874518
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.4±0.1 g/cm3
|
| Index of Refraction |
1.622
|
| LogP |
1.37
|
| Hydrogen Bond Donor Count |
10
|
| Hydrogen Bond Acceptor Count |
11
|
| Rotatable Bond Count |
20
|
| Heavy Atom Count |
47
|
| Complexity |
1110
|
| Defined Atom Stereocenter Count |
6
|
| SMILES |
CCC([C@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](N)CC(O)=O)=O)CCCNC(N)=N)=O)C(C)C)=O)CC1=CC=C(O)C=C1)=O)C(O)=O)C
|
| InChi Key |
UVPBVMCAVNABKX-GXYVSGTKSA-N
|
| InChi Code |
InChI=1S/C30H48N8O9/c1-5-16(4)24(29(46)47)38-27(44)21(13-17-8-10-18(39)11-9-17)36-28(45)23(15(2)3)37-26(43)20(7-6-12-34-30(32)33)35-25(42)19(31)14-22(40)41/h8-11,15-16,19-21,23-24,39H,5-7,12-14,31H2,1-4H3,(H,35,42)(H,36,45)(H,37,43)(H,38,44)(H,40,41)(H,46,47)(H4,32,33,34)/t16-,19-,20-,21-,23-,24-/m0/s1
|
| Chemical Name |
(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-carboxypropanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-3-methylbutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoic 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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| 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 | 1.5043 mL | 7.5216 mL | 15.0432 mL | |
| 5 mM | 0.3009 mL | 1.5043 mL | 3.0086 mL | |
| 10 mM | 0.1504 mL | 0.7522 mL | 1.5043 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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