| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg | |||
| Other Sizes |
| Targets |
(Sar1,Ile4·8)-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) mediating the physiological effects of angiotensin II. The sarcosine substitution at position 1 and isoleucine substitutions at positions 4 and 8 may alter receptor binding, selectivity, or stability. The peptide is used to study receptor activation, signaling, and structure-activity relationships.
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| ln Vitro |
(Sar1,Ile4,8)-Angiotensin II (30 μM; 30 minutes) enhances GSK3α/β phosphorylation and insulin-stimulated Akt expression in hepatocytes [1].
In vitro, (Sar1,Ile4·8)-Angiotensin II is used in receptor binding and functional assays to study angiotensin receptor pharmacology. The peptide may act as an agonist or antagonist depending on the receptor subtype. It is used in calcium mobilization, inositol phosphate accumulation, or cAMP assays in cells expressing AT1R or AT2R. The multiple substitutions allow investigation of how specific residues contribute to receptor recognition and activation. |
| ln Vivo |
In vivo, (Sar1,Ile4·8)-Angiotensin II is used to study the physiological effects of angiotensin receptor activation. As an angiotensin II analog with multiple substitutions, it may have altered vasoconstrictor or pressor effects. The peptide is used in cardiovascular research to investigate blood pressure regulation and receptor-mediated responses. Detailed in vivo data depend on the experimental model and dosing regimen.
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| Enzyme Assay |
In vitro receptor binding assays for (Sar1,Ile4·8)-Angiotensin II involve incubating the peptide with membrane preparations expressing angiotensin receptors (AT1R or AT2R). Radiolabeled angiotensin II is used as a tracer. Competition binding experiments determine binding affinity (IC50, Ki) for each receptor subtype. Assays are performed in buffer systems at physiological pH with protease inhibitors. The multiple substitutions allow assessment of how each residue contributes to binding specificity.
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| Cell Assay |
In vitro cell-based assays for (Sar1,Ile4·8)-Angiotensin II use cells expressing angiotensin receptors, such as HEK-293 cells transfected with AT1R or AT2R. 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. Comparisons with native angiotensin II and other analogs reveal structure-activity relationships.
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| Animal Protocol |
In vivo animal studies for (Sar1,Ile4·8)-Angiotensin II use rodent models for cardiovascular research. The peptide is administered via intravenous or intraperitoneal injection. Blood pressure is monitored by telemetry or tail-cuff methods. Renal function and fluid balance may be assessed. The peptide's effects are compared to native angiotensin II and other analogs to determine how the substitutions alter physiological activity.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of (Sar1,Ile4·8)-Angiotensin II are typical of peptide analogs. The multiple amino acid substitutions may confer increased resistance to enzymatic degradation compared to native angiotensin II, potentially prolonging half-life. As a peptide, it has limited oral bioavailability and is typically administered by injection. Detailed PK parameters require experimental determination.
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| Toxicity/Toxicokinetics |
Toxicity data for (Sar1,Ile4·8)-Angiotensin II are limited as it is a research peptide. Peptide analogs of angiotensin II 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 apply. Cardiovascular effects should be considered in experimental design.
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| References | |
| Additional Infomation |
(Sar1,Ile4·8)-Angiotensin II is a synthetic peptide analog with sarcosine at position 1 and isoleucine at positions 4 and 8. It is used to study angiotensin receptor pharmacology, structure-activity relationships, and signaling. The multiple substitutions allow investigation of how specific amino acid residues contribute to receptor recognition, activation, and metabolic stability. It is for research use only.
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| Molecular Formula |
C43H75N13O9
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|---|---|
| Molecular Weight |
918.13700
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| Exact Mass |
917.581
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| CAS # |
185461-45-4
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| PubChem CID |
101008474
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| Appearance |
White to off-white solid powder
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| LogP |
3.078
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| Hydrogen Bond Donor Count |
11
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| Hydrogen Bond Acceptor Count |
12
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| Rotatable Bond Count |
28
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| Heavy Atom Count |
65
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| Complexity |
1650
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| Defined Atom Stereocenter Count |
10
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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]([C@@H](C)CC)C(=O)O)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)CNC
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| InChi Key |
IOOIRDJKADTVNI-MMYICMJWSA-N
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| InChi Code |
InChI=1S/C43H75N13O9/c1-10-24(6)33(39(61)51-29(19-27-20-47-22-49-27)41(63)56-18-14-16-30(56)37(59)55-35(42(64)65)26(8)12-3)54-40(62)34(25(7)11-2)53-38(60)32(23(4)5)52-36(58)28(50-31(57)21-46-9)15-13-17-48-43(44)45/h20,22-26,28-30,32-35,46H,10-19,21H2,1-9H3,(H,47,49)(H,50,57)(H,51,61)(H,52,58)(H,53,60)(H,54,62)(H,55,59)(H,64,65)(H4,44,45,48)/t24-,25-,26-,28-,29-,30-,32-,33-,34-,35-/m0/s1
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| Chemical Name |
(2S,3S)-2-[[(2S)-1-[(2S)-2-[[(2S,3S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-5-(diaminomethylideneamino)-2-[[2-(methylamino)acetyl]amino]pentanoyl]amino]-3-methylbutanoyl]amino]-3-methylpentanoyl]amino]-3-methylpentanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]pyrrolidine-2-carbonyl]amino]-3-methylpentanoic 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) |
H2O : ~100 mg/mL (~108.92 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 | 1.0892 mL | 5.4458 mL | 10.8916 mL | |
| 5 mM | 0.2178 mL | 1.0892 mL | 2.1783 mL | |
| 10 mM | 0.1089 mL | 0.5446 mL | 1.0892 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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