| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 100mg | |||
| Other Sizes |
| Targets |
(Sar1)-Angiotensin II targets angiotensin receptors, specifically the angiotensin II type 1 receptor (AT1R) and type 2 receptor (AT2R). These are G protein-coupled receptors (GPCRs) that mediate the physiological effects of angiotensin II. The sarcosine substitution at position 1 may alter receptor binding affinity, selectivity, or metabolic stability compared to native angiotensin II. The peptide is used to study receptor activation, signaling, and pharmacology.
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| ln Vitro |
On days 5, 7, and 9, respectively, (Sar1)-Angiotensin II (1 μM/day; 9 days) raised the total protein content in embryonic chicken myocytes by 18.5, 26.2, and 22.2% [2]. Cynomolgus monkey brain meningeal-rich granules bind to (Sar1)-angiotensin II with a Kd of 2.7 nM [3].
In vitro, (Sar1)-Angiotensin II is used in receptor binding assays to study angiotensin receptor pharmacology. The peptide can act as an agonist or antagonist depending on the receptor subtype and experimental conditions. It is commonly used in functional assays such as calcium mobilization, inositol phosphate accumulation, or cAMP measurement in cells expressing AT1R or AT2R. The peptide's activity is compared to native angiotensin II to assess the effects of the sarcosine substitution. |
| ln Vivo |
In vivo, (Sar1)-Angiotensin II is used to study the physiological effects of angiotensin receptor activation. As an angiotensin II analog, it may have vasoconstrictor or pressor effects depending on its receptor selectivity and efficacy. The peptide is used in cardiovascular research to investigate blood pressure regulation, renal function, and fluid homeostasis. Detailed in vivo data for this specific analog would depend on the experimental model and dosing regimen.
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| Enzyme Assay |
In vitro receptor binding assays for (Sar1)-Angiotensin II involve incubating the peptide with membrane preparations expressing angiotensin receptors (AT1R or AT2R). Radiolabeled angiotensin II (e.g., 125I-angiotensin II) is used as a tracer. Competition binding experiments determine the peptide's binding affinity (IC50, Ki) for each receptor subtype. Assays are performed in buffer systems at physiological pH with appropriate protease inhibitors to prevent peptide degradation.
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| Cell Assay |
In vitro cell-based assays for (Sar1)-Angiotensin II use cells expressing angiotensin receptors, such as HEK-293 cells transfected with AT1R or AT2R, or native cells like vascular smooth muscle cells or adrenal cells. Cells are treated with the peptide at various concentrations. Functional responses measured include intracellular calcium mobilization (Fluo-4 or Fura-2), inositol phosphate accumulation, cAMP levels, or ERK phosphorylation. Dose-response curves determine EC50 or IC50 values for agonism or antagonism.
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| Animal Protocol |
In vivo animal studies for (Sar1)-Angiotensin II typically use rodent models to study cardiovascular and renal effects. The peptide is administered via intravenous or intraperitoneal injection. Blood pressure is monitored by telemetry or tail-cuff methods. Renal function is assessed by urine output and electrolyte excretion. Pharmacokinetic parameters may be determined from plasma samples. The peptide's effects are compared to native angiotensin II or receptor antagonists.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of (Sar1)-Angiotensin II are typical of peptide analogs. The sarcosine substitution at position 1 may confer increased resistance to enzymatic degradation compared to native angiotensin II, potentially prolonging its half-life. As a peptide, it has limited oral bioavailability and is typically administered by injection. Detailed PK parameters such as half-life, clearance, and volume of distribution would require experimental determination.
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| Toxicity/Toxicokinetics |
Toxicity data for (Sar1)-Angiotensin II are limited as it is a research peptide. Peptide analogs of angiotensin II are generally well-tolerated at research doses but may cause cardiovascular effects due to their vasoactive properties. The compound is for research use only and not for human therapeutic use. Standard laboratory safety precautions for peptide handling apply. Cardiovascular effects should be considered when designing in vivo experiments.
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| References |
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| Additional Infomation |
(Sar1)-Angiotensin II is a synthetic peptide analog of angiotensin II with sarcosine substitution at position 1. It is used as a research tool to study angiotensin receptor pharmacology, signaling, and physiology. The peptide is valuable for investigating the structure-activity relationships of angiotensin II and for developing receptor-selective ligands. It is used in cardiovascular and renal research. It is for research use only and not for human therapeutic or diagnostic use.
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| Molecular Formula |
C49H71N13O10
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|---|---|
| Molecular Weight |
1002.16914
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| Exact Mass |
1001.54
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| CAS # |
51833-69-3
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| PubChem CID |
10373777
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| Appearance |
White to off-white solid powder
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| LogP |
3.177
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| Hydrogen Bond Donor Count |
12
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| Hydrogen Bond Acceptor Count |
13
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| Rotatable Bond Count |
28
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| Heavy Atom Count |
72
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| Complexity |
1840
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| Defined Atom Stereocenter Count |
8
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| 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)NC(=O)CNC
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| InChi Key |
WCYZYYURIHACQW-KOTWUFNXSA-N
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| InChi Code |
InChI=1S/C49H71N13O10/c1-6-29(4)41(46(69)58-36(24-32-25-53-27-55-32)47(70)62-21-11-15-38(62)44(67)59-37(48(71)72)23-30-12-8-7-9-13-30)61-43(66)35(22-31-16-18-33(63)19-17-31)57-45(68)40(28(2)3)60-42(65)34(56-39(64)26-52-5)14-10-20-54-49(50)51/h7-9,12-13,16-19,25,27-29,34-38,40-41,52,63H,6,10-11,14-15,20-24,26H2,1-5H3,(H,53,55)(H,56,64)(H,57,68)(H,58,69)(H,59,67)(H,60,65)(H,61,66)(H,71,72)(H4,50,51,54)/t29-,34-,35-,36-,37-,38-,40-,41-/m0/s1
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| Chemical Name |
(2S)-2-[[(2S)-1-[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-(diaminomethylideneamino)-2-[[2-(methylamino)acetyl]amino]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
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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 (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)
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| 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
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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 | 0.9978 mL | 4.9892 mL | 9.9783 mL | |
| 5 mM | 0.1996 mL | 0.9978 mL | 1.9957 mL | |
| 10 mM | 0.0998 mL | 0.4989 mL | 0.9978 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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