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| Targets |
Neuromedin B targets the neuromedin B receptor (NMBR), a G protein-coupled receptor (GPCR) belonging to the bombesin receptor family. NMBR is activated by neuromedin B with high affinity and selectivity, although it can also be activated by other bombesin-like peptides such as gastrin-releasing peptide (GRP) with lower affinity. NMBR is expressed in various tissues, including the gastrointestinal tract, central nervous system, and smooth muscle. Upon activation by neuromedin B, NMBR couples to Gq/11 proteins, leading to phospholipase C activation, inositol trisphosphate production, and intracellular calcium mobilization. This signaling pathway mediates smooth muscle contraction, secretion, and neuronal excitation. Neuromedin B also modulates neurotransmitter release and has been implicated in the regulation of feeding behavior, thermoregulation, and stress responses. The peptide is a valuable tool for studying NMBR function and bombesin-related signaling.
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| ln Vitro |
The effects of Neuromedin B (NMB) and Bombesin (BN) on smooth muscle's smooth contractile were compared. When BN is used as a base, the relative effective price is determined to be 48% for GRP and 4.9% for NMB. On pancreatic strips, NMB likewise exhibits contractile activity, but its potency (peptide concentration ratio) only reaches 50% of the maximum response; about 5% of BN (BN/EC50 EC50 of NMB) and around 10% of GRP (GRP/EC50 EC50 of NMB) are accounted for by EC50 [1].
In vitro, Neuromedin B activates the neuromedin B receptor (NMBR) in cell-based assays, stimulating intracellular calcium mobilization and downstream signaling pathways. In NMBR-expressing cells (e.g., CHO-NMBR or HEK293-NMBR), treatment with Neuromedin B (1-100 nM) induces a rapid and transient increase in intracellular calcium, which can be measured using calcium-sensitive dyes such as Fluo-4 or Fura-2. Neuromedin B also stimulates ERK phosphorylation and other signaling pathways downstream of NMBR activation. The peptide exhibits potent agonist activity at NMBR with EC₅₀ values typically in the low nanomolar range. Neuromedin B has been used to study NMBR-mediated regulation of smooth muscle contraction, secretion, and neuronal activity in various cell and tissue preparations. These in vitro studies have established Neuromedin B as a key endogenous ligand for NMBR. |
| ln Vivo |
The effectiveness of NMB and GRP on fundus smooth muscle contraction was observed in both NMB-R-deficient and wild-type mice. The corresponding ED50 values for these two groups of mice were 10.9±2.3 (n=8) and 14.4±2.3 (n=8), respectively[1].
In vivo, Neuromedin B has been shown to regulate various physiological functions, including gastrointestinal motility, smooth muscle contraction, and feeding behavior. Administration of Neuromedin B to animals induces contraction of gastrointestinal smooth muscle, stimulates gastric acid secretion, and modulates pancreatic enzyme secretion. In the central nervous system, Neuromedin B has been implicated in the regulation of thermoregulation, stress responses, and feeding behavior. Intracerebroventricular administration of Neuromedin B in rodents has been shown to affect food intake and body temperature. The peptide also modulates neurotransmitter release in various brain regions. These in vivo findings demonstrate the physiological importance of Neuromedin B and its receptor NMBR in regulating gastrointestinal and neuronal functions. |
| Enzyme Assay |
In vitro receptor binding assays for Neuromedin B typically involve competition binding studies using radiolabeled Neuromedin B. A typical protocol: membrane preparations from NMBR-expressing cells (e.g., CHO-NMBR) are incubated with [¹²⁵I]-Neuromedin B (20-50 pM) and varying concentrations of unlabeled Neuromedin B (0.01 nM to 10 μM) in binding buffer (50 mM HEPES, pH 7.4, 5 mM MgCl₂, 0.1% BSA, 0.1 mM bacitracin) for 60-90 minutes at room temperature. Non-specific binding is determined in the presence of 1 μM unlabeled Neuromedin B. Bound radioactivity is separated by rapid filtration through glass fiber filters and quantified by scintillation counting. Kᵢ and Bmax values are calculated from competition curves using nonlinear regression. For functional assays, NMBR-expressing cells are loaded with Fluo-4 or Fura-2 AM, and calcium mobilization is measured upon stimulation with Neuromedin B (0.01-1000 nM) using a fluorescence microplate reader. EC₅₀ values are calculated from dose-response curves. Each concentration is tested in triplicate, and experiments are repeated at least three times.
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| Cell Assay |
In vitro cell-based assays for Neuromedin B are performed using NMBR-expressing cell lines such as CHO-NMBR, HEK293-NMBR, or NMBR-expressing native cells. A typical protocol: cells are seeded in 96-well black-walled clear-bottom plates at 20,000-50,000 cells/well and cultured overnight. Cells are loaded with Fluo-4 AM (2-5 μM) or Fura-2 AM (2-5 μM) in assay buffer (HBSS, 20 mM HEPES, pH 7.4, 0.1% BSA) for 30-60 minutes at 37°C. After washing, cells are stimulated with Neuromedin B at concentrations ranging from 0.01 to 1000 nM, and fluorescence is measured (excitation 485 nm, emission 525 nm for Fluo-4) using a fluorescence microplate reader. Calcium mobilization is expressed as relative fluorescence units or as a percentage of the maximum response. For ERK phosphorylation assays, cells are serum-starved for 2-4 hours, stimulated with Neuromedin B (1-100 nM) for 5-15 minutes, and lysed for phospho-ERK ELISA or Western blot. Each condition is tested in triplicate, and EC₅₀ values are calculated from dose-response curves.
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| Animal Protocol |
In vivo animal studies for Neuromedin B typically involve administration of the peptide to rodents via various routes. A typical protocol for gastrointestinal motility studies: male Sprague-Dawley rats are fasted overnight, then administered Neuromedin B via intraperitoneal or intravenous injection at doses of 1-100 μg/kg. Gastric emptying or intestinal transit is assessed by administering a fluorescent or radioactive marker and measuring its progression through the gastrointestinal tract. For smooth muscle contraction studies, tissues (e.g., ileum, colon) are isolated and mounted in organ baths, and Neuromedin B is added at concentrations of 0.1-1000 nM to measure contraction force. For central nervous system studies, Neuromedin B is administered via intracerebroventricular injection (1-10 μg) in rodents, and behavioral or physiological parameters (e.g., food intake, body temperature, locomotor activity) are monitored. Each study includes vehicle controls and appropriate positive controls.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Neuromedin B have not been fully characterized due to its nature as a peptide. As a decapeptide, Neuromedin B is susceptible to rapid degradation by peptidases in the gastrointestinal tract and plasma, resulting in poor oral bioavailability. The peptide has a short half-life in circulation, typically on the order of minutes, due to enzymatic degradation. Neuromedin B can cross the blood-brain barrier to some extent, but its brain penetration is limited. The peptide is typically administered via injection (intravenous, intraperitoneal, or intracerebroventricular) for in vivo studies. Its metabolism is primarily mediated by peptidases, including neutral endopeptidase and other proteolytic enzymes. The peptide should be stored at -20°C or -80°C for long-term stability and protected from repeated freeze-thaw cycles.
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| Toxicity/Toxicokinetics |
Pharmacokinetic properties of Neuromedin B have not been fully characterized due to its nature as a peptide. As a decapeptide, Neuromedin B is susceptible to rapid degradation by peptidases in the gastrointestinal tract and plasma, resulting in poor oral bioavailability. The peptide has a short half-life in circulation, typically on the order of minutes, due to enzymatic degradation. Neuromedin B can cross the blood-brain barrier to some extent, but its brain penetration is limited. The peptide is typically administered via injection (intravenous, intraperitoneal, or intracerebroventricular) for in vivo studies. Its metabolism is primarily mediated by peptidases, including neutral endopeptidase and other proteolytic enzymes. The peptide should be stored at -20°C or -80°C for long-term stability and protected from repeated freeze-thaw cycles.
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| References | |
| Additional Infomation |
Decapeptide isolated from porcine spinal cord
Toxicological data for Neuromedin B are limited as the peptide is a naturally occurring neuropeptide and research tool rather than a therapeutic agent. At physiological concentrations, Neuromedin B is well-tolerated and plays important roles in normal physiology. High doses of Neuromedin B may cause excessive smooth muscle contraction, gastrointestinal disturbances, or alterations in neuronal activity. The peptide has not undergone formal toxicology testing for regulatory purposes. Standard laboratory safety precautions should be followed when handling Neuromedin B: use of personal protective equipment (gloves, safety goggles, lab coat) and handling in a well-ventilated fume hood. The peptide should be stored at -20°C or -80°C and protected from light and moisture. No genotoxicity, carcinogenicity, or reproductive toxicity data are available. Researchers should consult the safety data sheet (SDS) before handling. |
| Molecular Formula |
C52H73N15O12S
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| Molecular Weight |
1132.29432
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| Exact Mass |
1131.53
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| CAS # |
87096-84-2
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| PubChem CID |
6324606
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| Appearance |
White to off-white solid powder
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| Density |
1.337 g/cm3
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| Boiling Point |
1697.4ºC
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| Flash Point |
980.3ºC
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| Index of Refraction |
1.613
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| LogP |
2.051
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| Hydrogen Bond Donor Count |
15
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| Hydrogen Bond Acceptor Count |
15
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| Rotatable Bond Count |
33
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| Heavy Atom Count |
80
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| Complexity |
2140
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| Defined Atom Stereocenter Count |
9
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| SMILES |
C[C@H]([C@@H](C(=O)NCC(=O)N[C@@H](CC1=CN=CN1)C(=O)N[C@@H](CC2=CC=CC=C2)C(=O)N[C@@H](CCSC)C(=O)N)NC(=O)[C@H](C)NC(=O)[C@H](CC3=CNC4=CC=CC=C43)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)N)NC(=O)CN)O
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| InChi Key |
YPFNACALNKVZNK-MFNIMNRCSA-N
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| InChi Code |
InChI=1S/C52H73N15O12S/c1-27(2)17-36(64-51(78)40(21-41(54)69)61-42(70)22-53)48(75)66-38(19-31-23-57-34-14-10-9-13-33(31)34)47(74)60-28(3)46(73)67-44(29(4)68)52(79)58-25-43(71)62-39(20-32-24-56-26-59-32)50(77)65-37(18-30-11-7-6-8-12-30)49(76)63-35(45(55)72)15-16-80-5/h6-14,23-24,26-29,35-40,44,57,68H,15-22,25,53H2,1-5H3,(H2,54,69)(H2,55,72)(H,56,59)(H,58,79)(H,60,74)(H,61,70)(H,62,71)(H,63,76)(H,64,78)(H,65,77)(H,66,75)(H,67,73)/t28-,29+,35-,36-,37-,38-,39-,40-,44-/m0/s1
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| Chemical Name |
(2S)-2-[(2-aminoacetyl)amino]-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-4-methylsulfanyl-1-oxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]butanediamide
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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) |
H2O : ~12.5 mg/mL (~11.04 mM)
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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 | 0.8832 mL | 4.4158 mL | 8.8317 mL | |
| 5 mM | 0.1766 mL | 0.8832 mL | 1.7663 mL | |
| 10 mM | 0.0883 mL | 0.4416 mL | 0.8832 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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