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| 5mg |
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| Targets |
Bradykinin (1-7) is a fragment of the full-length bradykinin peptide (1-9). The primary target of bradykinin is the bradykinin B2 receptor, a G protein-coupled receptor that mediates the vasoactive and inflammatory effects of bradykinin. As a truncated peptide, Bradykinin (1-7) may have reduced affinity for the B2 receptor compared to full-length bradykinin, but it is still able to interact with bradykinin receptors and modulate their activity. The peptide is also a substrate for endopeptidase, which cleaves it from the full-length peptide. Bradykinin (1-7) is used to study the structure-activity relationships of bradykinin and its metabolites.
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| ln Vitro |
Bradykinin is a tissue-based system that has strong effects on the heart and kidneys. A highly sensitive amino-terminal directed radioimmunoassay that detects bradykinin-(1-7), bradykinin-(1-8) using high-performance liquid chromatography, and bradykinin-(1-9) was created in order to examine the regulation of this system. Bradykinin was identified using carboxyl-terminal guided radioimmunoassay in rat kidney and blood. Bradykinin-(1-9) (~100 fmol/g tissue wet weight) and Bradykinin-(1-7) (~70 fmol/g) are the two main bradykinin peptides found in the kidney. Of these, Bradykinin-(1-8) is detectable (~8 fmol/g) and Bradykinin-(4-9) (~12 fmol/g); Bradykinin-(2-9) and Bradykinin-(3-9) are below the detection limit. Bradykinin-(1–9) is only found in blood at extremely low concentrations (~2 fmol/ml), and the detection limit for other bradykinin peptides is exceeded. The angiotensin-converting enzyme (ACE) inhibitor perindopril administered with renal levels of bradykinin-1–8, bradykinin–9, and bradykinin–(1–7) roughly triples as well as reduces correlation. Bradykinin:(1–9) proportion. The aorta, adrenal glands, brain, adrenal glands, heart, and brown adipose tissue can all be treated with N-terminal guided radioimmunoassay. Bradykinin-(1-7) and bradykinin-(1-9) abundances for these tissues are comparable (16-340 fmol/g), although levels of bradykinin-(1-8) are lower[1].
In vitro, Bradykinin (1-7) is a metabolite of bradykinin that is used as a research tool to study the bradykinin system. It is used to study the specificity and kinetics of kininases, the enzymes that degrade bradykinin. The peptide is also used as an external calibrant or standard in MALDI-TOF mass spectrometry analysis. Its biological activity is related to its ability to interact with bradykinin receptors, although its affinity and potency are lower than those of the full-length peptide. Bradykinin (1-7) is a valuable tool for studying the bradykinin signaling pathway and for developing new therapeutic agents targeting this system. |
| ln Vivo |
In vivo, Bradykinin is a tissue-based system that has strong effects on the heart and kidneys. Bradykinin dilates blood vessels via the release of prostacyclin, nitric oxide, and endothelium-derived hyperpolarizing factor. As a metabolite of bradykinin, Bradykinin (1-7) may have some of these in vivo effects, although its potency is reduced compared to the full-length peptide. The compound is used in research to study the metabolism and function of bradykinin in vivo. A highly sensitive amino-terminal directed radioimmunoassay has been developed to detect bradykinin-(1-7) using high-performance liquid chromatography.
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| Enzyme Assay |
The in vitro binding activity of Bradykinin (1-7) can be assessed using receptor binding assays with the bradykinin B2 receptor. A typical protocol involves incubating the peptide with membranes from cells expressing the B2 receptor and a radiolabeled bradykinin ligand (e.g., [3H]-bradykinin). Bound and free ligand are separated by filtration, and the radioactivity is measured. The IC50 or Ki value is determined by plotting the percentage of specific binding remaining against the peptide concentration. The activity of the peptide can also be assessed using functional assays, such as measuring calcium mobilization or inositol phosphate accumulation in cells expressing the B2 receptor.
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| Cell Assay |
For in vitro cellular experiments, cells expressing the bradykinin B2 receptor (e.g., endothelial cells, smooth muscle cells, or transfected cell lines) are cultured in appropriate media and treated with Bradykinin (1-7) at various concentrations (typically 0.1-100 microM). The peptide's ability to activate the B2 receptor is assessed by measuring downstream signaling, such as calcium mobilization using fluorescent calcium indicators (e.g., Fluo-4) or inositol phosphate accumulation using a radiolabeled assay. The duration of treatment varies depending on the specific assay. The peptide can also be used in competition assays with full-length bradykinin to determine its relative affinity and potency.
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| Animal Protocol |
In vivo animal experiments with Bradykinin (1-7) are not commonly performed, as it is a metabolite of bradykinin. However, the peptide can be administered to animals (e.g., rats or mice) via intravenous or intraperitoneal injection to study its effects on blood pressure, vascular permeability, or other physiological parameters. A typical protocol involves administering the peptide at various doses (e.g., 0.1-10 mg/kg) and measuring hemodynamic parameters using telemetry or tail-cuff methods. Blood samples are collected to measure the levels of the peptide and its metabolites using highly sensitive radioimmunoassays. The peptide is also used as a standard in analytical methods for measuring bradykinin and its metabolites in biological samples.
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| ADME/Pharmacokinetics |
Bradykinin (1-7) is a peptide with a molecular weight of 756.85 g/mol and a molecular formula of C35H52N10O9. As a peptide, its pharmacokinetic properties are characterized by rapid clearance from the circulation due to proteolytic degradation. The peptide is typically administered by injection in preclinical studies. Its half-life is short, and it is rapidly metabolized by peptidases in the blood and tissues. The peptide is stable in lyophilized form and should be stored at -20degC. It is soluble in water and aqueous buffers. Its pharmacokinetic properties make it suitable for acute pharmacological studies but less suitable for chronic dosing.
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| Toxicity/Toxicokinetics |
Bradykinin (1-7) is a peptide fragment of bradykinin and is generally considered to have low toxicity. As a naturally occurring peptide, it is expected to be well-tolerated at pharmacological doses. However, high doses may cause hypotension or other effects due to its vasoactive properties. The compound should be handled with standard laboratory precautions and is intended for research use only.
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| References | |
| Additional Infomation |
[des-Phe(8), des-Arg(9)]-bradykinin is a heptapeptide composed of Arg, Pro, Pro, Gly, Phe, Ser, and Pro residues linked sequentially by peptide bonds. It is a metabolite of bradykinin, lacking the Phe residue at position 8 and the Arg residue at position 9. It is a metabolite from both humans and rats. It is the conjugate base of [des-Phe(8), des-Arg(9)]-bradykinin(1+).
Bradykinin (1-7) is an amino-truncated peptide fragment derived from bradykinin. It is a metabolite of bradykinin, formed by enzymatic cleavage by endopeptidase. Bradykinin is a pro-inflammatory mediator and neuromediator. Bradykinin (1-7) is used as a research tool to study the bradykinin system and the specificity and kinetics of kininases. It is also used as an external calibrant or standard in MALDI-TOF mass spectrometry. The peptide is available as a research compound and is not approved for clinical use. |
| Molecular Formula |
C35H52N10O9
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|---|---|
| Molecular Weight |
756.84898
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| Exact Mass |
756.392
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| CAS # |
23815-87-4
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| PubChem CID |
168145
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| Appearance |
White to off-white solid powder
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| Density |
1.52 g/cm3
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| Index of Refraction |
1.695
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| LogP |
-4.7
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| Hydrogen Bond Donor Count |
8
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
17
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| Heavy Atom Count |
54
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| Complexity |
1400
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| Defined Atom Stereocenter Count |
6
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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)O
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| InChi Key |
CRROPKNGCGVIOG-QCOJBMJGSA-N
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| InChi Code |
InChI=1S/C35H52N10O9/c36-22(10-4-14-39-35(37)38)31(50)44-16-6-12-26(44)33(52)43-15-5-11-25(43)30(49)40-19-28(47)41-23(18-21-8-2-1-3-9-21)29(48)42-24(20-46)32(51)45-17-7-13-27(45)34(53)54/h1-3,8-9,22-27,46H,4-7,10-20,36H2,(H,40,49)(H,41,47)(H,42,48)(H,53,54)(H4,37,38,39)/t22-,23-,24-,25-,26-,27-/m0/s1
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| Chemical Name |
(2S)-1-[(2S)-2-[[(2S)-2-[[2-[[(2S)-1-[(2S)-1-[(2S)-2-amino-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carbonyl]amino]acetyl]amino]-3-phenylpropanoyl]amino]-3-hydroxypropanoyl]pyrrolidine-2-carboxylic 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) |
H2O : ~100 mg/mL (~132.13 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (132.13 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.3213 mL | 6.6063 mL | 13.2127 mL | |
| 5 mM | 0.2643 mL | 1.3213 mL | 2.6425 mL | |
| 10 mM | 0.1321 mL | 0.6606 mL | 1.3213 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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