| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Bradykinin (1-5) targets the bradykinin B2 receptor, which is a G protein-coupled receptor. However, as a metabolite fragment, it may exhibit reduced affinity compared to the full-length bradykinin peptide. It can inhibit platelet aggregation induced by α-thrombin and γ-thrombin. Its interactions with kinin receptors make it a useful tool for studying the bradykinin signaling pathway and its role in cardiovascular and inflammatory processes.
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| ln Vitro |
In vitro, Bradykinin (1-5) can inhibit platelet aggregation induced by α-thrombin and γ-thrombin. This activity distinguishes it from full-length bradykinin, which is a potent vasodilator. As a stable metabolite, it is often used in analytical studies to monitor bradykinin metabolism and ACE activity. Its biological activity is primarily related to its interactions with bradykinin receptors and its role in the kinin-kallikrein system.
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| ln Vivo |
Bradykinin is a short-lived vasoactive peptide with a reported in vivo half-life of 17 seconds and is rapidly converted to bradykinin in the circulation (1-5). Bradykinin (1-5) is the result of two sequential cleavages of bradykinin by ACE at the Pro7-Phe8 and Phe5-Ser6 links. It has been discovered as the primary stable metabolite of bradykinin in human beings. The last half-life is minutes. Both bradykinin and bradykinin(1-5) reduced α- and γ-thrombin-induced platelet aggregation (P<0.01 compared with baseline). Bradykinin(1-5) reduces gamma-thrombin-induced platelet aggregation by 50% at an estimated dose of 183±3 pmol/min. Neither bradykinin nor bradykinin(1-5) affects thrombin receptor activating peptide-induced platelet aggregation, consistent with bradykinin and bradykinin(1-5) functioning by blocking thrombin receptor cleavage and thrombin receptor release to suppress thrombin-induced platelet aggregation. Activating peptides. Bradykinin (1-5) significantly attenuates α-thrombin-induced platelet aggregation but not TRAP 1-6-induced platelet aggregation. Bradykinin (1-5) substantially suppresses platelet aggregation induced by γ-thrombin (500 nM) with an ED50 of 183±2 pmol/min[1].
In vivo, Bradykinin is a short-lived vasoactive peptide with a half-life of approximately 17 seconds, and its metabolite Bradykinin (1-5) serves as a stable marker for bradykinin turnover. While the metabolite itself has reduced vasoactive properties compared to the parent peptide, it can still influence platelet function and other physiological processes. Its stability makes it a valuable research tool for studying bradykinin metabolism. |
| Enzyme Assay |
In vitro receptor binding assays for Bradykinin (1-5) typically involve radioligand displacement studies using membrane preparations from cells expressing bradykinin B2 receptors. The compound's affinity for the receptor is determined by measuring its ability to displace a specific radiolabeled ligand, such as [3H]-bradykinin. These cell-free assays provide a direct measure of the peptide's binding affinity for the bradykinin receptor.
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| Cell Assay |
In vitro cellular assays for Bradykinin (1-5) assess its functional activity at bradykinin receptors. Cells expressing the B2 receptor are treated with the peptide, and downstream signaling, such as calcium mobilization or nitric oxide production, is measured. Its ability to inhibit platelet aggregation is assessed in platelet-rich plasma or washed platelet preparations stimulated with thrombin.
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| Animal Protocol |
In vivo animal studies for Bradykinin (1-5) are not extensively detailed in the literature, as the compound is primarily used as a research tool for studying bradykinin metabolism and as an analytical standard. It may be used in pharmacokinetic studies to track bradykinin turnover or in models of inflammation to assess the role of the kinin-kallikrein system.
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| ADME/Pharmacokinetics |
Bradykinin is a short-lived vasoactive peptide with a half-life in vivo of approximately 17 seconds. Bradykinin (1-5), as its major stable metabolite, is formed by ACE-mediated proteolysis and serves as a useful marker for bradykinin metabolism. The peptide has a molecular formula of C27H40N8O6 and a molecular weight of 572.66.
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| Toxicity/Toxicokinetics |
Specific toxicity data for Bradykinin (1-5) are not extensively detailed in the available literature, as it is a research compound and a naturally occurring metabolite. Its toxicity is likely related to its pharmacological activity at bradykinin receptors, but comprehensive toxicological studies are not typically conducted for such research-use peptides. It is not intended for therapeutic use.
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| References | |
| Additional Infomation |
Bradykinin (1-5) (CAS 23815-89-6) is a stable N-terminal pentapeptide fragment of bradykinin, formed by the proteolytic action of ACE. It can inhibit platelet aggregation induced by α-thrombin and γ-thrombin. With a molecular formula of C27H40N8O6 and a molecular weight of 572.66, it is used as a research tool for studying bradykinin metabolism, ACE activity, and platelet function. It is not approved for clinical use.
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| Molecular Formula |
C27H40N8O6
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| Molecular Weight |
572.6565
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| Exact Mass |
572.307
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| CAS # |
23815-89-6
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| PubChem CID |
3081453
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| Appearance |
White to off-white solid powder
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| Density |
1.46g/cm3
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| Index of Refraction |
1.677
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| LogP |
1.036
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
13
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| Heavy Atom Count |
41
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| Complexity |
981
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| Defined Atom Stereocenter Count |
4
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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)O
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| InChi Key |
USSUMSBPLJWFSZ-TUFLPTIASA-N
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| InChi Code |
InChI=1S/C27H40N8O6/c28-18(9-4-12-31-27(29)30)24(38)35-14-6-11-21(35)25(39)34-13-5-10-20(34)23(37)32-16-22(36)33-19(26(40)41)15-17-7-2-1-3-8-17/h1-3,7-8,18-21H,4-6,9-16,28H2,(H,32,37)(H,33,36)(H,40,41)(H4,29,30,31)/t18-,19-,20-,21-/m0/s1
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| Chemical Name |
(2S)-2-[[2-[[(2S)-1-[(2S)-1-[(2S)-2-amino-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carbonyl]amino]acetyl]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, 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) |
DMSO : ~100 mg/mL (~174.62 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.37 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.37 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.37 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7462 mL | 8.7312 mL | 17.4624 mL | |
| 5 mM | 0.3492 mL | 1.7462 mL | 3.4925 mL | |
| 10 mM | 0.1746 mL | 0.8731 mL | 1.7462 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05304091 | Unknown status | Other: Questionnaire on a smartphone application | Bradykinin-mediated Angioedema | University Hospital, Lille | 2022-08 | |
| NCT00780637 | Withdrawn | Drug: Bradykinin | Heart Transplantation | Vanderbilt University | 2008-10 | Not Applicable |
| NCT00780481 | Terminated | Drug: Bradykinin | Obesity | Vanderbilt University | 2007-01 | Not Applicable |
| NCT00965393 | Completed | Procedure: Forearm vascular study Drug: Placebo Drug: bradykinin receptor antagonist (HOE-140) |
Ischaemic Heart Diseases | University of Edinburgh | 2009-08 | Not Applicable |
| NCT01091116 | Completed | Drug: MEN16132 - 0.125 mg Drug: MEN16132 - 0.25 mg Drug: MEN16132 - 0.5 mg |
Osteoarthritis, Knee | Menarini Group | 2010-03 | Phase 2 |
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