| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Bradykinin (2-9) targets the bradykinin B2 receptor. It binds to the receptor and activates it, leading to the activation of downstream signaling pathways, including phospholipase C, calcium mobilization, and nitric oxide production. It has lower affinity than full-length bradykinin.
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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 (2-9) induces vasodilation, increases vascular permeability, and stimulates the release of prostaglandins and other inflammatory mediators. It also stimulates pain nerve endings. It is less potent than bradykinin but retains significant activity. |
| ln Vivo |
In vivo, bradykinin (2-9) has been shown to induce hypotension, increase vascular permeability, and cause pain when administered to animals. It is used to study the role of the kinin system in inflammation and pain.
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| Enzyme Assay |
Bradykinin B2 receptor binding assays are performed using membranes from cells expressing the B2 receptor. Radiolabeled bradykinin is used as a tracer. Various concentrations of bradykinin (2-9) are added, and bound radioactivity is measured. Ki values are calculated from competition binding curves.
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| Cell Assay |
Cells expressing the B2 receptor (e.g., HEK293 cells transfected with B2R) are cultured. Cells are loaded with a calcium-sensitive fluorescent dye, and changes in intracellular calcium are measured upon addition of bradykinin (2-9). The EC50 is calculated from the dose-response curve.
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| Animal Protocol |
Animal studies use rodent models. Bradykinin (2-9) is administered via intravenous, intra-arterial, or intradermal injection. Blood pressure is measured. Vascular permeability is assessed by Evans blue extravasation. Pain is assessed by measuring withdrawal responses.
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| ADME/Pharmacokinetics |
Bradykinin (2-9) is a peptide (sequence PPGFRSSR, MW 902.02) that is rapidly metabolized by peptidases. It has a short half-life in vivo. It is typically administered by injection.
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| Toxicity/Toxicokinetics |
Bradykinin (2-9) is generally well-tolerated at pharmacologically active doses. No significant toxicity has been reported. It is a research compound and not intended for human use.
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| References | |
| Additional Infomation |
Bradykinin (2-9) is a research tool used to study the kinin system. It is not an approved drug and is not in clinical trials. It is a fragment of bradykinin, also known as bradykinin (2-9) or des-Arg1-bradykinin.
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| Molecular Formula |
C44H61N11O10
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|---|---|
| Molecular Weight |
904.02300
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| Exact Mass |
903.46
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| CAS # |
16875-11-9
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| PubChem CID |
14694060
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| Appearance |
White to off-white solid powder
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| Density |
1.47g/cm3
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| Index of Refraction |
1.684
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| LogP |
0.951
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| Hydrogen Bond Donor Count |
10
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| Hydrogen Bond Acceptor Count |
12
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| Rotatable Bond Count |
22
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| Heavy Atom Count |
65
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| Complexity |
1700
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| Defined Atom Stereocenter Count |
7
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| SMILES |
C1C[C@H](NC1)C(=O)N2CCC[C@H]2C(=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=CC=C5)C(=O)N[C@@H](CCCN=C(N)N)C(=O)O
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| InChi Key |
ZZHVXIPXTCBVBE-POFDKVPJSA-N
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| InChi Code |
InChI=1S/C44H61N11O10/c45-44(46)48-20-8-16-30(43(64)65)51-38(59)32(24-28-13-5-2-6-14-28)52-40(61)35-18-10-22-55(35)42(63)33(26-56)53-37(58)31(23-27-11-3-1-4-12-27)50-36(57)25-49-39(60)34-17-9-21-54(34)41(62)29-15-7-19-47-29/h1-6,11-14,29-35,47,56H,7-10,15-26H2,(H,49,60)(H,50,57)(H,51,59)(H,52,61)(H,53,58)(H,64,65)(H4,45,46,48)/t29-,30-,31-,32-,33-,34-,35-/m0/s1
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| Chemical Name |
(2S)-5-(diaminomethylideneamino)-2-[[(2S)-2-[[(2S)-1-[(2S)-3-hydroxy-2-[[(2S)-3-phenyl-2-[[2-[[(2S)-1-[(2S)-pyrrolidine-2-carbonyl]pyrrolidine-2-carbonyl]amino]acetyl]amino]propanoyl]amino]propanoyl]pyrrolidine-2-carbonyl]amino]-3-phenylpropanoyl]amino]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) |
DMSO : ~100 mg/mL (~110.62 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.77 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 (2.77 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 (2.77 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 | 1.1062 mL | 5.5309 mL | 11.0617 mL | |
| 5 mM | 0.2212 mL | 1.1062 mL | 2.2123 mL | |
| 10 mM | 0.1106 mL | 0.5531 mL | 1.1062 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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