| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Lys-(Des-Arg9)-Bradykinin targets the bradykinin B1 receptor (B1R) with high selectivity. It has Ki values of 0.12 nM for human B1, 1.7 nM for mouse B1, and 0.23 nM for rabbit B1 receptors. The compound has low inhibitory activity on B2 receptors, with a Ki of >30000 nM for human B2. It is 16-fold more potent than [Des-Arg9]-Bradykinin.
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| ln Vitro |
Lys-[Des-Arg9]Bradykinin activates through the bradykinin B1 receptor (B1R) and is momentarily produced through the potential of bradykinin [1]. Lys-[Des-Arg9]Bradykinin (Lda-BK; 10 μM) is an IL-12p70-dependent factor that increases IL-12p40 in hMo-DC. It was demonstrated that Lys-[Des-Arg9] bradykinin can limit the chemotaxis of saturated hMo-DC by using Lys-[Des-Arg9]Bradykinin-dependent migration of hMo-DC [1].
In vitro, Lys-(Des-Arg9)-Bradykinin activates the bradykinin B1 receptor (B1R). It is an IL-12p70-dependent factor that increases IL-12p40 in human monocyte-derived dendritic cells (hMo-DC) at 10 μM. The compound's high selectivity and potency for B1 over B2 receptors make it a valuable tool for studying B1 receptor-mediated signaling. |
| ln Vivo |
Although lipopolysaccharide-induced peripheral vascular resistance in rabbits can be lessened with Lys-[Des-Arg9]Bradykinin (1 μg; intranasal injection; New Zealand white rabbit) therapy, the impact is transient (T1/2=118-195 s) [3].
In vivo, Lys-(Des-Arg9)-Bradykinin is used to study bradykinin B1 receptor-mediated effects. Its high selectivity and potency for B1 receptors allow researchers to dissect the physiological and pathophysiological roles of B1 receptor activation. The compound has been studied in models of inflammation, pain, and vascular function. Its effects are mediated through B1 receptor activation, leading to downstream signaling events. |
| Enzyme Assay |
For non-cellular assays, Lys-(Des-Arg9)-Bradykinin is evaluated for its binding affinity to bradykinin B1 and B2 receptors using radioligand binding assays. Receptor binding is assessed using membrane preparations from cells expressing human, mouse, or rabbit B1 receptors. Ki values are determined from competition binding experiments. Selectivity for B1 over B2 receptors is confirmed by comparing binding affinities.
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| Cell Assay |
In vitro cell culture experiments are performed using cells expressing bradykinin B1 receptors, such as human monocyte-derived dendritic cells (hMo-DC). Cells are treated with Lys-(Des-Arg9)-Bradykinin at concentrations ranging from 0.1 nM to 10 μM. Endpoints include receptor activation (calcium flux, IP3 production), downstream signaling (MAPK activation), and cytokine production (IL-12p40, IL-12p70). The compound's activity is compared to other bradykinin receptor agonists and antagonists.
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| Animal Protocol |
In vivo animal studies are conducted in mouse, rat, and rabbit models. Lys-(Des-Arg9)-Bradykinin is administered intravenously, intraperitoneally, or locally. Pharmacodynamic endpoints include blood pressure changes, vascular permeability, pain responses, and inflammatory markers. The compound's effects are compared to those of B1 receptor antagonists to confirm receptor specificity. Tissue distribution and receptor occupancy are assessed in target organs.
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| ADME/Pharmacokinetics |
Lys-(Des-Arg9)-Bradykinin has a molecular weight of approximately 1032.20 Da. It is a peptide with the sequence Lys-Arg-Pro-Pro-Gly-Phe-Ser-Pro-Phe (lacking Arg9). The peptide is typically stored as a lyophilized powder and reconstituted in appropriate buffers for experimental use. Pharmacokinetic properties are characteristic of peptides, with rapid clearance and limited oral bioavailability. It is stable under recommended storage conditions.
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| Toxicity/Toxicokinetics |
Toxicological profiles of Lys-(Des-Arg9)-Bradykinin are not well characterized. As a naturally occurring peptide, it is expected to have low toxicity at physiological concentrations. Standard laboratory safety precautions should be followed during handling. The compound is for research use only and is not intended for therapeutic applications.
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| References |
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| Additional Infomation |
Lys-(Des-Arg9)-Bradykinin is a naturally occurring kinin and a potent, highly selective bradykinin B1 receptor agonist. It has Ki values of 0.12 nM (human B1), 1.7 nM (mouse B1), and 0.23 nM (rabbit B1) with low B2 activity. It is used as a research tool to study B1 receptor signaling and inflammatory pathways and is for research use only.
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| Molecular Formula |
C50H73N13O11
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|---|---|
| Molecular Weight |
1032.19512
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| Exact Mass |
1031.56
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| CAS # |
71800-36-7
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| PubChem CID |
122227
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.45g/cm3
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| Index of Refraction |
1.678
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| LogP |
1.656
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| Hydrogen Bond Donor Count |
11
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| Hydrogen Bond Acceptor Count |
14
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| Rotatable Bond Count |
27
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| Heavy Atom Count |
74
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| Complexity |
1960
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| Defined Atom Stereocenter Count |
8
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| SMILES |
OC[C@@H](C(N1CCC[C@H]1C(N[C@H](C(O)=O)CC2=CC=CC=C2)=O)=O)NC([C@@H](NC(CNC([C@@H]3CCCN3C([C@@H]4CCCN4C([C@@H](NC([C@@H](N)CCCCN)=O)CCCNC(N)=N)=O)=O)=O)=O)CC5=CC=CC=C5)=O
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| InChi Key |
AILVBOHFGXNHCC-TZPCGENMSA-N
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| InChi Code |
InChI=1S/C50H73N13O11/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/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)/t33-,34-,35-,36-,37-,38-,39-,40-/m0/s1
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| 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
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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 |
| 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 | 0.9688 mL | 4.8440 mL | 9.6880 mL | |
| 5 mM | 0.1938 mL | 0.9688 mL | 1.9376 mL | |
| 10 mM | 0.0969 mL | 0.4844 mL | 0.9688 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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