![Lys-[Des-Arg9]Bradykinin TFA](/upload/1124/V75329.png)
| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| Other Sizes |
| Targets |
Bradykinin B1 Receptor (B1R)
Targets the bradykinin B1 receptor (B1R) with very high selectivity and affinity. It acts as a potent agonist, displaying Ki values of 0.12 nM for the human receptor, 1.7 nM for the mouse receptor, and 0.23 nM for the rabbit receptor. It has low inhibitory activity on the B2 receptor, making it a highly specific B1R probe. |
|---|---|
| ln Vitro |
Lys-[Des-Arg9]Bradykinin TFA activates via the bradykinin B1 receptor (B1R) and is produced by proteolytic cleavage of bradykinin [1]. Lys-[Des-Arg9]Bradykinin TFA (Lda-BK; 10 μM) stimulates mature hMo-DCs' release of IL-12p70 while suppressing their secretion of IL-12p40. [1] Lys-[Des-Arg9] bradykinin may block the chemokines of mature hMo-DCs, as pretreatment decreased the migration of mature hMo-DCs to culture medium alone.
As a potent B1 receptor agonist, Lys-[Des-Arg9]Bradykinin activates B1R-mediated signaling pathways, including G-protein coupling, phospholipase C activation, and calcium mobilization. At a concentration of 10 uM, it has been shown to enhance the secretion of IL-12p70 and inhibit the secretion of IL-12p40 by mature human monocyte-derived dendritic cells (hMo-DCs), demonstrating its role in modulating immune responses. |
| ln Vivo |
Although the impact is transient (T1/2 is 118-195 seconds), Lys-[Des-Arg9]Bradykinin TFA (1 μg; intra-arterial injection; New Zealand white rabbit) therapy can lessen LPS-induced peripheral vascular resistance in rabbits [3].
In vivo, Lys-[Des-Arg9]Bradykinin is used to activate the B1 receptor in animal models to study its effects on blood pressure, pain sensitivity (hyperalgesia), and inflammation. Its activity is often assessed by measuring induced paw edema or hyperalgesia in rodents, and the effects can be blocked by co-administration of a selective B1 receptor antagonist like R715. |
| Enzyme Assay |
Non-cell radioligand binding assays are performed using membranes from cells expressing human, mouse, or rabbit B1 receptors. The membranes are incubated with a radiolabeled B1 receptor agonist (e.g., [3H]Lys-des-Arg9-bradykinin) and increasing concentrations of the unlabeled test compound. Bound radioactivity is separated by filtration and counted to determine the Ki values.
|
| Cell Assay |
Functional cell-based assays are performed in primary human monocyte-derived dendritic cells (hMo-DCs). The cells are treated with the peptide (e.g., 10 uM) for a standard period. Supernatants are then collected and the concentrations of secreted cytokines, such as IL-12p70 and IL-12p40, are measured by ELISA to assess the functional consequences of B1 receptor activation.
|
| Animal Protocol |
No specific animal studies for this agonist are reported. In typical inflammation models, an intraplantar injection of this agonist into the hind paw of a rodent can be used to induce B1 receptor-mediated edema and hyperalgesia. Paw swelling is measured using a plethysmometer, and pain sensitivity is assessed using von Frey filaments, providing a functional readout for the B1 receptor pathway in vivo.
|
| ADME/Pharmacokinetics |
Detailed pharmacokinetic data is not publicly available. As a naturally occurring peptide, it is rapidly degraded in vivo by proteolytic enzymes, leading to a short half-life. For in vivo experiments, it is typically administered locally via injection to achieve a local effect rather than systemic exposure.
|
| Toxicity/Toxicokinetics |
No specific toxicity data is available for Lys-[Des-Arg9]Bradykinin. As an endogenous agonist peptide, it is part of the kinin system and is generally not considered toxic in its physiological context. However, its potent pro-inflammatory and pain-inducing effects mean that it can cause significant discomfort and tissue responses when administered in research settings.
|
| References |
|
| Additional Infomation |
Lys-[Des-Arg9]Bradykinin TFA is a research-grade peptide and is not approved for clinical use. It is an indispensable, highly selective pharmacological tool for identifying and characterizing the bradykinin B1 receptor and for studying its role in inflammatory diseases, pain transmission, and immune cell modulation.
|
| Molecular Formula |
C52H74F3N13O13
|
|---|---|
| Molecular Weight |
1146.21848249435
|
| Exact Mass |
1145.548
|
| CAS # |
2763588-90-3
|
| PubChem CID |
145707527
|
| Appearance |
White to off-white solid powder
|
| Hydrogen Bond Donor Count |
12
|
| Hydrogen Bond Acceptor Count |
19
|
| Rotatable Bond Count |
27
|
| Heavy Atom Count |
81
|
| Complexity |
2040
|
| Defined Atom Stereocenter Count |
8
|
| SMILES |
C1C[C@H](N(C1)C(=O)[C@@H]2CCCN2C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CCCCN)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=CC=C5)C(=O)O.C(=O)(C(F)(F)F)O
|
| InChi Key |
BUNFBEBTCVIRNN-HVJIRRSLSA-N
|
| InChi Code |
InChI=1S/C50H73N13O11.C2HF3O2/c51-22-8-7-17-33(52)42(66)58-34(18-9-23-55-50(53)54)46(70)63-26-12-21-40(63)48(72)62-25-10-19-38(62)44(68)56-29-41(65)57-35(27-31-13-3-1-4-14-31)43(67)60-37(30-64)47(71)61-24-11-20-39(61)45(69)59-36(49(73)74)28-32-15-5-2-6-16-32;3-2(4,5)1(6)7/h1-6,13-16,33-40,64H,7-12,17-30,51-52H2,(H,56,68)(H,57,65)(H,58,66)(H,59,69)(H,60,67)(H,73,74)(H4,53,54,55);(H,6,7)/t33-,34-,35-,36-,37-,38-,39-,40-;/m0./s1
|
| Chemical Name |
(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[2-[[(2S)-1-[(2S)-1-[(2S)-2-[[(2S)-2,6-diaminohexanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carbonyl]amino]acetyl]amino]-3-phenylpropanoyl]amino]-3-hydroxypropanoyl]pyrrolidine-2-carbonyl]amino]-3-phenylpropanoic acid;2,2,2-trifluoroacetic acid
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO: 110 mg/mL (95.97 mM)
H2O: 50 mg/mL (43.62 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.75 mg/mL (2.40 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 27.5 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: ≥ 2.75 mg/mL (2.40 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 27.5 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: ≥ 2.75 mg/mL (2.40 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (87.24 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.8724 mL | 4.3622 mL | 8.7243 mL | |
| 5 mM | 0.1745 mL | 0.8724 mL | 1.7449 mL | |
| 10 mM | 0.0872 mL | 0.4362 mL | 0.8724 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
