![[Sar1, Ile8]-Angiotensin II TFA (AngiotensinII TFA; Angiotensin 2 TFA)](/upload/1124/V77338.png)
| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
Angiotensin II receptors (AT1 and AT2). Unlike native angiotensin II, which is a full agonist, [Sar1, Ile8]-Angiotensin II acts as a potent antagonist at AT1 receptors. It is a classic and widely used angiotensin receptor antagonist (saralasin analog) in cardiovascular research. It exhibits high affinity for both AT1 and AT2 receptors, effectively blocking the vasoconstrictive and aldosterone-secreting effects of angiotensin II by competitive inhibition.
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| ln Vitro |
In addition to contracting healthy arteries, [Sar1, Ile8]-Angiotensin II(TFA) can cause hypertrophy or hyperplasia in cultured cells or illness-related vasculature. Vascular smooth muscle cells are stimulated to produce superoxide anion production and both NADPH and NADH oxidases are activated by [Sar1, Ile8]-Angiotensin II(TFA)[1].
In vitro, [Sar1, Ile8]-Angiotensin II TFA has multiple effects on vascular smooth muscle, including contraction of normal arteries and hypertrophy or hyperplasia of cultured cells or diseased vessels. It activates both the NADPH and NADH oxidases and stimulates superoxide anion formation in vascular smooth muscle cells. Although classified as an antagonist, studies show it exhibits partial agonism, stimulating inositol phosphate production in mutant AT1 receptors, indicating residual agonist activity. |
| ln Vivo |
In vivo, [Sar1, Ile8]-Angiotensin II TFA serves as a partial antagonist of the renin-angiotensin system. In animal models, it blocks the pressor response to angiotensin II and reduces blood pressure. It is used to elucidate the role of AT1 and AT2 receptors in physiological processes. The [Sar1,Ile8] analog exhibits a characteristically long duration of action compared to other antagonists, possibly due to binding to a different site on the angiotensin receptor.
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| Enzyme Assay |
A non-cell radioligand binding assay is used to determine receptor affinity. Membranes from CHO cells expressing human AT1 or AT2 receptors are incubated with the radioligand [125I]-Sar1,Ile8-Angiotensin II (a high-affinity tracer) in the presence of varying concentrations of unlabeled peptide. After incubation at room temperature for 60 minutes, the mixture is filtered through GF/B filters to separate bound from free ligand. The radioactivity is counted, and the Ki is calculated using the Cheng-Prusoff equation.
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| Cell Assay |
For cellular signaling studies, primary vascular smooth muscle cells (VSMCs) are seeded in 6-well plates and serum-starved. Cells are treated with varying concentrations of [Sar1, Ile8]-Angiotensin II TFA (0.1 nM to 10 uM) for 5-30 minutes. The activation of intracellular signaling cascades is assessed by Western blot for phosphorylated ERK1/2, p38 MAPK, and PLC-gamma. Superoxide anion production is measured by the reduction of cytochrome c or by using a chemiluminescent probe like lucigenin.
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| Animal Protocol |
In vivo experiments to test angiotensin antagonists are performed in normotensive or hypertensive rat models. Animals are anesthetized, and the carotid artery is cannulated for blood pressure measurement via a pressure transducer. The jugular vein is cannulated for intravenous drug administration. A submaximal dose of angiotensin II (e.g., 100 ng/kg) is administered IV to establish a baseline pressor response. Then, a bolus of [Sar1, Ile8]-Angiotensin II TFA (10-100 ug/kg) is administered 5-10 minutes before a repeat angiotensin II challenge to measure the blockade of the pressor response.
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| ADME/Pharmacokinetics |
[Sar1, Ile8]-Angiotensin II TFA is soluble in H2O and DMSO. For in vitro cell studies, it is dissolved in sterile saline or cell culture media. For in vivo IV administration, it is dissolved in sterile saline (0.9% NaCl). The peptide has a short plasma half-life (minutes) due to rapid enzymatic degradation by peptidases. The TFA salt improves solubility, making it easier to formulate at high concentrations for in vivo experiments. Storage: -80degC for long-term, away from moisture.
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| Toxicity/Toxicokinetics |
The TFA salt is non-toxic at the concentrations used for research. The safety profile of angiotensin receptor antagonists is well-established. In animal experiments, the peptide is well-tolerated at the doses used to block the renin-angiotensin system (e.g., 10-100 ug/kg IV). The primary off-target effects are related to its partial agonist activity and the physiological consequences of blocking the RAS (e.g., hypotension, natriuresis). No significant acute toxicity has been reported in the literature at standard research doses.
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| References | |
| Additional Infomation |
[Sar1, Ile8]-Angiotensin II TFA is a research-grade chemical, not a clinical drug, and is used exclusively as a pharmacological tool. It is a classic control or reference compound in receptor pharmacology studies investigating the structure-activity relationships (SAR) of the renin-angiotensin system. The analog is critical for mapping receptor binding sites, investigating competitive inhibition, and understanding the pharmacodynamics of peptide-receptor engagement. This product is for research use only (RUO).
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| Molecular Formula |
C48H74F3N13O12
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| Molecular Weight |
1082.18
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| Related CAS # |
[Sar1, Ile8]-Angiotensin II;37827-06-8
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| Appearance |
Typically exists as solid at room temperature
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
H2O :~50 mg/mL (~46.20 mM)
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| 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 | 0.9241 mL | 4.6203 mL | 9.2406 mL | |
| 5 mM | 0.1848 mL | 0.9241 mL | 1.8481 mL | |
| 10 mM | 0.0924 mL | 0.4620 mL | 0.9241 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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