| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| 100mg | |||
| Other Sizes |
| Targets |
(Tyr8)-Bradykinin targets bradykinin receptors, specifically the bradykinin B2 receptor (BDKRB2) and to a lesser extent the B1 receptor (BDKRB1). These are G protein-coupled receptors (GPCRs) that mediate the biological effects of bradykinin. The tyrosine substitution at position 8 provides a site for radioiodination, allowing the peptide to be used as a radioligand for receptor binding and autoradiography studies.
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|---|---|
| ln Vitro |
[Tyr8]Bradykinin (10 nM, 2 min) raises phosphorylated ERK1/2 quickly [1].
In vitro, (Tyr8)-Bradykinin is used in receptor binding assays to study bradykinin receptor pharmacology. As a radioiodinated ligand (125I-(Tyr8)-Bradykinin), it is used for saturation binding experiments to determine receptor density (Bmax) and binding affinity (Kd). Competition binding experiments with unlabeled ligands determine Ki values. The peptide is also used in functional assays such as calcium mobilization to assess its agonist or antagonist activity at bradykinin receptors. |
| ln Vivo |
In vivo, (Tyr8)-Bradykinin is used in receptor imaging and distribution studies. Radioiodinated (Tyr8)-Bradykinin can be used for autoradiography to localize bradykinin receptors in tissues. The peptide may also be used in pharmacokinetic studies to assess the distribution and clearance of bradykinin analogs. As a bradykinin analog, it may have vasodilatory or hypotensive effects depending on its receptor activity.
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| Enzyme Assay |
In vitro receptor binding assays for (Tyr8)-Bradykinin involve incubating radioiodinated peptide (125I-(Tyr8)-Bradykinin) with membrane preparations expressing bradykinin receptors (B2 or B1). Saturation binding experiments determine Kd and Bmax. Competition binding experiments with unlabeled ligands determine Ki values. Assays are performed in buffer systems at physiological pH with protease inhibitors. Nonspecific binding is determined in the presence of excess unlabeled bradykinin.
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: Serum-depleted Trabecular Mesh Cells Tested Concentrations: 10 nM Incubation Duration: 2 minutes Experimental Results: Phosphorylated ERK1/2 increased rapidly, with a magnitude comparable to that observed with bradykinin. In vitro cell-based assays for (Tyr8)-Bradykinin use cells expressing bradykinin receptors, such as endothelial cells, smooth muscle cells, or transfected HEK-293 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, nitric oxide production, or ERK phosphorylation. Dose-response curves determine EC50 or IC50 values. The tyrosine substitution may slightly alter receptor activity compared to native bradykinin. |
| Animal Protocol |
In vivo animal studies for (Tyr8)-Bradykinin use rodent models for cardiovascular and inflammatory research. The peptide is administered via intravenous or intraperitoneal injection. Blood pressure is monitored by telemetry or tail-cuff methods. Radiolabeled peptide can be used for biodistribution studies to assess tissue distribution and receptor occupancy. The peptide's effects are compared to native bradykinin to determine how tyrosine substitution affects activity.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of (Tyr8)-Bradykinin are typical of peptide analogs. Bradykinin and its analogs have very short half-lives in circulation due to rapid degradation by kininases. The tyrosine substitution may allow radioiodination but does not substantially alter the rapid clearance of the peptide. 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 (Tyr8)-Bradykinin are limited as it is a research peptide. Bradykinin analogs may cause hypotension, increased vascular permeability, and pain due to their vasoactive and pro-inflammatory properties. The compound is for research use only and not for human therapeutic use. Radiolabeled forms require appropriate radiation safety precautions. Standard laboratory safety precautions apply.
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| References |
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| Additional Infomation |
(Tyr8)-Bradykinin is a synthetic peptide analog of bradykinin with tyrosine at position 8 for radioiodination. It is used as a radioligand for bradykinin receptor binding studies, autoradiography, and receptor localization. Bradykinin receptors are involved in inflammation, pain, and cardiovascular regulation. The peptide is for research use only.
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| Molecular Formula |
C50H73N15O12
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|---|---|
| Molecular Weight |
1076.21000
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| Exact Mass |
1075.56
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| CAS # |
32222-00-7
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| PubChem CID |
5018571
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| Appearance |
White to off-white solid powder
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| LogP |
0.986
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| Hydrogen Bond Donor Count |
13
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| Hydrogen Bond Acceptor Count |
15
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| Rotatable Bond Count |
27
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| Heavy Atom Count |
77
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| Complexity |
2110
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1C[C@H](N(C1)C(=O)[C@@H]2CCCN2C(=O)[C@H](CCCN=C(N)N)N)C(=O)NCC(=O)N[C@@H](CC3=CC=CC=C3)C(=O)N[C@@H](CO)C(=O)N4CCC[C@H]4C(=O)N[C@@H](CC5=CC=C(C=C5)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)O
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| InChi Key |
MWVUEDATXZGOMI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C50H73N15O12/c51-32(11-4-20-56-49(52)53)45(73)65-24-8-15-39(65)47(75)64-23-6-13-37(64)43(71)58-27-40(68)59-34(25-29-9-2-1-3-10-29)41(69)62-36(28-66)46(74)63-22-7-14-38(63)44(72)61-35(26-30-16-18-31(67)19-17-30)42(70)60-33(48(76)77)12-5-21-57-50(54)55/h1-3,9-10,16-19,32-39,66-67H,4-8,11-15,20-28,51H2,(H,58,71)(H,59,68)(H,60,70)(H,61,72)(H,62,69)(H,76,77)(H4,52,53,56)(H4,54,55,57)
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| Chemical Name |
2-[[2-[[1-[2-[[2-[[2-[[1-[1-[2-amino-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carbonyl]amino]acetyl]amino]-3-phenylpropanoyl]amino]-3-hydroxypropanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-5-(diaminomethylideneamino)pentanoic 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, 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) |
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 | 0.9292 mL | 4.6459 mL | 9.2919 mL | |
| 5 mM | 0.1858 mL | 0.9292 mL | 1.8584 mL | |
| 10 mM | 0.0929 mL | 0.4646 mL | 0.9292 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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