| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| Other Sizes |
| Targets |
(Lys3)-Bombesin targets bombesin receptors, specifically the gastrin-releasing peptide receptor (GRPR) and neuromedin B receptor (NMBR). These are G protein-coupled receptors (GPCRs) that mediate the biological effects of bombesin-like peptides. The lysine residue at position 3 provides a functional group for conjugation to labels, fluorophores, or chelators for imaging or therapeutic applications while maintaining receptor-binding activity.
|
|---|---|
| ln Vitro |
In vitro, (Lys3)-Bombesin is used in receptor binding and functional assays to study bombesin receptor pharmacology. The peptide binds to GRPR and NMBR with high affinity. It is commonly used in calcium mobilization assays, inositol phosphate accumulation, or proliferation assays in cells expressing bombesin receptors. The lysine at position 3 allows for conjugation to fluorescent dyes or radiolabels for imaging or detection purposes.
|
| ln Vivo |
In vivo, (Lys3)-Bombesin is used in preclinical imaging and therapeutic studies targeting bombesin receptors. Radiolabeled or fluorescently labeled (Lys3)-Bombesin analogs are used for tumor imaging, as bombesin receptors are overexpressed in various cancers including prostate, breast, and lung cancer. The peptide is also used to study the physiological effects of bombesin receptor activation in animal models.
|
| Enzyme Assay |
In vitro receptor binding assays for (Lys3)-Bombesin involve incubating the peptide with membrane preparations expressing bombesin receptors (GRPR or NMBR). Radiolabeled bombesin is used as a tracer. Competition binding experiments determine binding affinity (IC50, Ki). The lysine at position 3 does not significantly impair receptor binding, making it suitable for conjugation. Assays are performed in buffer systems at physiological pH with protease inhibitors.
|
| Cell Assay |
In vitro cell-based assays for (Lys3)-Bombesin use cells expressing bombesin receptors, such as PC-3 prostate cancer cells or transfected HEK-293 cells. Cells are treated with the peptide at various concentrations. Functional responses measured include intracellular calcium mobilization (Fluo-4 or Fura-2), inositol phosphate accumulation, or cell proliferation. Dose-response curves determine EC50 values. Fluorescently labeled analogs can be used for receptor internalization and imaging studies.
|
| Animal Protocol |
In vivo animal studies for (Lys3)-Bombesin typically use tumor xenograft models expressing bombesin receptors. Radiolabeled or fluorescently labeled (Lys3)-Bombesin is administered intravenously for imaging studies (PET, SPECT, or optical imaging). Biodistribution and tumor uptake are assessed. For therapeutic studies, cytotoxic conjugates may be evaluated. The peptide may also be used to study bombesin's physiological effects on gastrointestinal function, thermoregulation, or satiety in rodent models.
|
| ADME/Pharmacokinetics |
Pharmacokinetic properties of (Lys3)-Bombesin are typical of peptide receptor-targeting agents. As a small peptide, it has rapid clearance from circulation, limited oral bioavailability, and susceptibility to proteolytic degradation. The lysine at position 3 allows for conjugation to imaging or therapeutic payloads, which can alter PK properties. For imaging applications, rapid clearance is often desirable for high target-to-background ratios.
|
| Toxicity/Toxicokinetics |
Toxicity data for (Lys3)-Bombesin are limited as it is a research peptide. Peptide analogs targeting bombesin receptors are generally well-tolerated at research doses. The compound is for research use only and not for human therapeutic or diagnostic use without appropriate regulatory approvals. Standard laboratory safety precautions for peptide handling apply.
|
| Additional Infomation |
(Lys3)-Bombesin is a synthetic peptide analog of bombesin with lysine at position 3 for conjugation purposes. It is used as a research tool for bombesin receptor studies, including receptor binding, signaling, and imaging applications. Bombesin receptors are overexpressed in various cancers, making this peptide valuable for tumor targeting and imaging research. It is for research use only and not for human therapeutic or diagnostic use.
|
| Molecular Formula |
C71H110N22O18S
|
|---|---|
| Molecular Weight |
1591.8347
|
| Exact Mass |
1590.81
|
| CAS # |
66839-66-5
|
| PubChem CID |
16132913
|
| Appearance |
Typically exists as solid at room temperature
|
| LogP |
2.973
|
| Hydrogen Bond Donor Count |
21
|
| Hydrogen Bond Acceptor Count |
21
|
| Rotatable Bond Count |
51
|
| Heavy Atom Count |
112
|
| Complexity |
3300
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C1(=CNC2C=CC=CC1=2)C[C@@H](C(=O)N[C@@H](C)C(=O)N[C@@H](C(C)C)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N)CCSC)CC1N=CNC=1)NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](CC(=O)N)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H]1NC(=O)CC1
|
| 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 |
| 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) |
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
|
|---|---|
| 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 | 0.6282 mL | 3.1410 mL | 6.2820 mL | |
| 5 mM | 0.1256 mL | 0.6282 mL | 1.2564 mL | |
| 10 mM | 0.0628 mL | 0.3141 mL | 0.6282 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
