| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 100mg | |||
| Other Sizes |
| Targets |
The primary targets of Bombesin are the bombesin receptors (BBRs), which are G-protein coupled receptors. It binds to the gastrin-releasing peptide receptor (GRPR) in rat pancreatic acinar cells with a Ki of 1.88 nM. It also binds to frog bombesin receptor subtype 4 (BB4) in CHO cells overexpressing the receptor with a Ki of 1.7 nM. It has a Ki of 3.20E+3 nM for the rat GRPR. By binding to these receptors, Bombesin activates downstream signaling pathways that regulate various physiological functions, including gastrointestinal hormone release and smooth muscle contraction.
|
|---|---|
| ln Vitro |
Gastrin-releasing peptide (GRP) and neuregulin are two mammalian bombesin-related peptides that have been linked to bombesin, a tetradecapeptide with a COOH terminus ending in Gly-His-Leu-Met-NH2. Very similar is B (NMB) [1]. It was discovered that bombesin stimulated the release of gastrointestinal hormones, the contraction of the gallbladder, the secretions from the stomach and pancreas, and bronchoconstriction. It is found in the brains of birds as well as in the stomach endocrine cells of amphibians and avian species. It is mostly present in nerve cells and fibers in mammals. P cells in the developing lung are the only known mammalian endocrine cells to contain bombesin. The mammalian brain contains bombesin as well, with the hypothalamus having the highest concentrations [2]. It was demonstrated that bombesin was a strong mitogen for Swiss 3T3 cells. Bombesin promotes 3T3 cell division when serum is present in low concentrations (3.5%). Bombesin induces DNA synthesis (IC50=1 nM) in serum-free medium without the need for additional growth factors [3].
In vitro, Bombesin binds to the gastrin-releasing peptide receptor (GRPR) in rat pancreatic acinar cells with a Ki of 1.88 nM. It also binds to frog bombesin receptor subtype 4 (BB4) in CHO cells with a Ki of 1.7 nM. It is a potent stimulator of gastric and pancreatic secretions and the release of gastrointestinal hormones in cell-based assays. Its activity is mediated through G-protein coupled receptor activation, leading to downstream signaling events such as calcium mobilization and mitogen-activated protein kinase (MAPK) activation. |
| ln Vivo |
In vivo, Bombesin has stimulatory effects on gastric and pancreatic secretions. It also exhibits antiepileptic/anticonvulsant potential. As a GRP analog, it stimulates intestinal function. Its effects on the central nervous system and gastrointestinal tract make it a valuable tool for studying these systems. It is used in research to investigate the physiological roles of bombesin-like peptides and their receptors.
|
| Enzyme Assay |
Cell-free receptor binding assays for Bombesin typically use membrane preparations from cells expressing bombesin receptors, such as rat pancreatic acinar cells or CHO cells overexpressing BB4. A standard protocol involves incubating the membranes with a radiolabeled ligand, such as [125I]-Tyr4-bombesin, and varying concentrations of unlabeled Bombesin. Bound and free ligand are separated by filtration, and the radioactivity is measured. The binding affinity (Ki) is determined from competitive displacement curves.
|
| Cell Assay |
For in vitro cellular experiments, cells expressing bombesin receptors (e.g., rat pancreatic acinar cells, CHO-BB4 cells) are cultured in appropriate media. Cells are treated with Bombesin at various concentrations (typically 0.1-1000 nM). Receptor activation is assessed by measuring intracellular calcium mobilization using fluorescent calcium indicators (e.g., Fluo-4). Alternatively, inositol phosphate accumulation can be measured using a radiolabeled assay. The EC50 is calculated from the dose-response curve.
|
| Animal Protocol |
In vivo animal experiments with Bombesin are typically conducted in rodents to study its effects on gastrointestinal function and the central nervous system. A common protocol involves administering the peptide via intravenous (IV) or intracerebroventricular (ICV) injection at various doses (e.g., 1-100 ug/kg). Its effects on gastric acid secretion, pancreatic enzyme release, and gut motility are measured. For anticonvulsant studies, it is administered in seizure models, and the latency to seizure onset is recorded.
|
| ADME/Pharmacokinetics |
Bombesin is a tetradecapeptide with a molecular weight of 1619.85 g/mol and a molecular formula of C71H112N24O18S. As a peptide, it is administered by injection in experimental settings. Its half-life in vivo is short due to proteolytic degradation. It is stable as a powder and should be stored at -20degC. It is soluble in aqueous buffers. Its pharmacokinetic properties are consistent with those of a peptide, characterized by rapid clearance.
|
| Toxicity/Toxicokinetics |
The toxicity profile of Bombesin is not extensively characterized, as it is a research tool. At the doses used in experiments, it is generally well-tolerated. However, its potent effects on gastrointestinal and neural functions mean that high doses can cause significant physiological effects. The compound is for research use only and not for human therapeutic use. It should be handled with standard laboratory precautions.
|
| References | |
| Additional Infomation |
Bombesin is being investigated in the clinical trial NCT01205321 (which aims to evaluate the radiation dosimetry, plasma pharmacokinetics, biodistribution, safety and tolerability, and diagnostic performance of BAY86-7548 in prostate cancer patients and healthy volunteers using PET/CT imaging). Bombesin is a fourteen-dose peptide originally extracted from the skin of the bell toad (Bombina bombina) and the variegata bell toad (B. variegata). It is also an endogenous neurotransmitter in many animals, including mammals. Bombesin affects blood vessels and other smooth muscle, gastric secretion, and renal circulation and function.
Bombesin is a tetradecapeptide originally isolated from amphibian skin that acts as an analog of gastrin-releasing peptide (GRP). It binds to bombesin receptors with high affinity (Ki = 1.88 nM for GRPR) and plays a key role in the release of gastrin and the activation of G-protein coupled receptors. It has stimulatory effects on gastric and pancreatic secretions and exhibits anticonvulsant potential. It is a valuable research tool for studying neuropeptide signaling. |
| Molecular Formula |
C71H110N24O18S.2[HCL]
|
|---|---|
| Molecular Weight |
1692.76998
|
| Exact Mass |
1618.82
|
| CAS # |
31362-50-2
|
| PubChem CID |
16201612
|
| Appearance |
White to off-white solid powder
|
| Density |
1.5g/cm3
|
| Index of Refraction |
1.681
|
| LogP |
2.598
|
| Hydrogen Bond Donor Count |
23
|
| Hydrogen Bond Acceptor Count |
21
|
| Rotatable Bond Count |
52
|
| Heavy Atom Count |
114
|
| Complexity |
3410
|
| Defined Atom Stereocenter Count |
12
|
| SMILES |
C[C@@H](C(=O)N[C@@H](C(C)C)C(=O)NCC(=O)N[C@@H](CC1=CN=CN1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N)NC(=O)[C@H](CC2=CNC3=CC=CC=C32)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](CCCNC(=N)N)NC(=O)[C@H](CCC(=O)N)NC(=O)[C@@H]4CCC(=O)N4
|
| InChi Key |
QXZBMSIDSOZZHK-DOPDSADYSA-N
|
| InChi Code |
InChI=1S/C71H110N24O18S/c1-34(2)24-47(92-62(105)43(14-11-22-79-71(76)77)89-64(107)45(15-18-52(72)96)90-63(106)44-17-20-55(99)85-44)61(104)81-31-56(100)87-51(28-54(74)98)69(112)91-46(16-19-53(73)97)65(108)94-49(26-38-29-80-41-13-10-9-12-40(38)41)66(109)84-37(7)60(103)95-58(36(5)6)70(113)82-32-57(101)86-50(27-39-30-78-33-83-39)68(111)93-48(25-35(3)4)67(110)88-42(59(75)102)21-23-114-8/h9-10,12-13,29-30,33-37,42-51,58,80H,11,14-28,31-32H2,1-8H3,(H2,72,96)(H2,73,97)(H2,74,98)(H2,75,102)(H,78,83)(H,81,104)(H,82,113)(H,84,109)(H,85,99)(H,86,101)(H,87,100)(H,88,110)(H,89,107)(H,90,106)(H,91,112)(H,92,105)(H,93,111)(H,94,108)(H,95,103)(H4,76,77,79)/t37-,42-,43-,44-,45-,46-,47-,48-,49-,50-,51-,58-/m0/s1
|
| Chemical Name |
(2S)-N-[(2S)-1-[[(2S)-1-[[2-[[(2S)-4-amino-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-4-methylsulfanyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-2-oxoethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]-2-[[(2S)-5-oxopyrrolidine-2-carbonyl]amino]pentanediamide
|
| 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) |
H2O : ~50 mg/mL (~30.87 mM)
|
|---|---|
| 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 | 0.5907 mL | 2.9537 mL | 5.9075 mL | |
| 5 mM | 0.1181 mL | 0.5907 mL | 1.1815 mL | |
| 10 mM | 0.0591 mL | 0.2954 mL | 0.5907 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
