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| 10mg |
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| Targets |
BIM 23042 TFA selectively targets the neuromedin B receptor (NMB-R), also known as BB1, which is a G protein-coupled receptor belonging to the bombesin receptor family. The compound acts as a competitive antagonist at this receptor, blocking neuromedin B-induced signaling. It has approximately 100-fold lower affinity for the gastrin-releasing peptide receptor (GRP-R, BB2), indicating excellent selectivity for the NMB receptor subtype. Neuromedin B receptors are involved in various physiological processes including regulation of body temperature, feeding behavior, circadian rhythms, and nociceptive signaling. By selectively blocking NMB-R, BIM 23042 serves as a valuable pharmacological tool for dissecting the specific roles of neuromedin B signaling in these processes, distinguishing it from GRP-mediated effects.
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| ln Vitro |
In vitro, BIM 23042 TFA inhibits Ca2+ release induced by neuromedin B, ICI 216140, and DPDM-bombesin acetamide in cells expressing the human neuromedin B receptor. The compound's antagonist activity has been characterized in receptor binding and functional assays using cells transfected with human neuromedin B receptors. BIM 23042 exhibits high affinity for NMB-R with approximately 100-fold selectivity over GRP-R. In functional assays, the compound effectively blocks neuromedin B-induced calcium mobilization, which is a key downstream signaling event following NMB receptor activation. These in vitro studies have established BIM 23042 as a reference antagonist for studying NMB receptor pharmacology and for distinguishing NMB-mediated effects from those mediated by other bombesin receptor family members.
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| ln Vivo |
In vivo activity of BIM 23042 TFA has been investigated in the context of nociceptive signaling. Studies have demonstrated a role for neuromedin B in pain modulation, and BIM 23042 has been used as a tool to explore this function. However, detailed in vivo efficacy data, including specific animal models, dosing regimens, and quantitative outcomes, are not extensively reported in the available literature. The compound is primarily used as a research tool for in vitro pharmacological characterization rather than for extensive in vivo efficacy studies. Its utility in vivo would be to block NMB-R signaling to assess the physiological roles of neuromedin B in various biological processes. Specific animal studies using BIM 23042 would involve administration via appropriate routes (e.g., intravenous, intraperitoneal) and evaluation of endpoints related to the biological process under investigation.
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| Enzyme Assay |
In vitro enzyme or receptor binding assay protocols for BIM 23042 TFA typically involve radioligand binding competition assays using membranes from cells expressing recombinant human neuromedin B receptors. A standard protocol would include incubating varying concentrations of BIM 23042 (typically 0.1 nM to 10 μM) with radiolabeled neuromedin B or a related ligand (e.g., 125I-neuromedin B) and receptor-containing membranes in binding buffer for a defined period (e.g., 60-120 minutes at room temperature). Non-specific binding is determined in the presence of excess unlabeled ligand. Bound radioactivity is separated by filtration or centrifugation and quantified by scintillation counting. IC50 values are calculated from competition curves, and Ki values are derived using the Cheng-Prusoff equation. Functional antagonist activity can be assessed by measuring inhibition of neuromedin B-induced Ca2+ mobilization in cells loaded with fluorescent calcium indicators.
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| Cell Assay |
In vitro cell-based assay protocols for BIM 23042 TFA typically involve measuring the compound's ability to inhibit neuromedin B-induced signaling in cells expressing the human neuromedin B receptor. A standard protocol would use cells (e.g., CHO or HEK293 cells stably transfected with human NMB-R) seeded in 96-well plates and loaded with a calcium-sensitive fluorescent dye such as Fluo-4. Cells are pre-incubated with varying concentrations of BIM 23042 (typically 0.1 nM to 10 μM) for 10-30 minutes, followed by stimulation with a submaximal concentration of neuromedin B (e.g., EC80). Fluorescence changes reflecting intracellular calcium elevation are measured using a fluorescence plate reader. The inhibition of calcium response is plotted against compound concentration to generate IC50 values. Alternatively, receptor internalization assays or downstream signaling readouts such as MAP kinase activation can be employed. Appropriate controls include vehicle-treated and neuromedin B-only stimulated cells.
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| Animal Protocol |
In vivo animal experimental protocols using BIM 23042 TFA have been reported in the context of studying nociceptive signaling pathways. In one study, the compound was used to investigate the role of neuromedin B in pain modulation. A typical protocol might involve administering BIM 23042 to rodents via intracerebroventricular (ICV) or intrathecal (IT) injection at doses determined from preliminary studies (e.g., 1-10 nmol per animal). Following administration, nociceptive responses are assessed using standard pain models such as the tail-flick test, hot plate test, or formalin-induced paw licking. The compound's effects are compared to vehicle controls and positive controls (e.g., morphine). For systemic administration, the compound can be formulated using standard injection formulations such as DMSO:Tween 80:Saline or DMSO:PEG300:Tween 80:Saline. Endpoints include latency to response, pain score, or other relevant behavioral measures.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of BIM 23042 TFA have not been extensively characterized in published studies. As a peptide analogue (octapeptide with a molecular weight of ~1192 Da for the free base), the compound would be expected to have limited oral bioavailability due to poor intestinal permeability and susceptibility to proteolytic degradation. Following parenteral administration, the compound would likely distribute into tissues and be cleared through proteolytic metabolism and renal excretion. The TFA salt form enhances solubility compared to the free base, with solubility in water of approximately 6 mg/mL with sonication. However, specific PK parameters such as half-life, Cmax, AUC, volume of distribution, and clearance have not been reported. The compound's stability requires storage under sealed, protected conditions away from moisture and light. Further pharmacokinetic studies would be needed to characterize its absorption, distribution, metabolism, and excretion profile.
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| Toxicity/Toxicokinetics |
Toxicological data for BIM 23042 TFA are limited, as the compound is intended for research use only and has not undergone systematic toxicity testing. No acute toxicity (LD50), subchronic toxicity, genotoxicity, or reproductive toxicity studies have been reported specifically for this compound. Based on its structure as a peptide analogue, the compound would be expected to have relatively low systemic toxicity due to rapid proteolytic degradation and clearance. However, as with all research chemicals, appropriate safety precautions should be taken when handling the compound, including working in a fume hood, wearing appropriate personal protective equipment, and avoiding inhalation, ingestion, or skin contact. The compound is not intended for human use. Researchers should consult the material safety data sheet (MSDS) for specific safety information and handling recommendations.
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| References | |
| Additional Infomation |
BIM 23042 TFA is a research-grade peptide antagonist used as a pharmacological tool for studying neuromedin B receptor (NMB-R, BB1) signaling. It was developed as a substituted somatostatin analogue with selectivity for NMB-R over GRP-R (approximately 100-fold). The compound inhibits neuromedin B-induced Ca2+ release and has been used in studies investigating the nociceptive signaling role of neuromedin B. BIM 23042 has not entered clinical trials and is not approved for any therapeutic indication. Its mechanism of action involves competitive antagonism at the NMB receptor, blocking the binding of neuromedin B and downstream signaling events. The compound is available exclusively for research purposes and is not intended for diagnostic, therapeutic, or human applications. Its selectivity profile makes it a valuable tool for distinguishing NMB-mediated effects from those mediated by GRP-R in bombesin receptor family research.
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| Molecular Formula |
C63H73N11O9S2.XC2HF3O2
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| Molecular Weight |
1192.45 (free base)
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| Appearance |
White to off-white solid powder
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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 (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)
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| Solubility (In Vitro) |
H2O :~6 mg/mL (with sonication)
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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.) |
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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