| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg | |||
| 500mg | |||
| Other Sizes |
Purity: =98.8%
| Targets |
BEL targets calcium-independent phospholipase A2 (iPLA2β). It acts as an irreversible and selective inhibitor with an IC50 of approximately 7 μM. It also inhibits Mg-dependent phosphatidate phosphatase (PAP). The (R)-BEL and (S)-BEL enantiomers exhibit approximately 10-fold selectivity for iPLA2γ and iPLA2β, respectively.
|
|---|---|
| ln Vitro |
RBL 2H3 and mast cells generated from bone marrow require Ca2+ entrance in order to undergo exocytosis (BMMC). When stimulated with the Ca2+ ionophore A23187, which passively transfers Ca2+ along the concentration gradient, as well as in permeabilized mast cells where Ca2+ entrance is no longer significant, bromoenolactone suppresses exocytosis. Moreover, bromoenolide very slightly affects the release of internal stores and prolonged increases in Ca2+ influx that are part of the Ca2+ signaling pathway that is triggered by antigens or thapsigargin [1].
In vitro, BEL inhibits iPLA2β with an IC50 of approximately 7 μM. It inhibits antigen-stimulated mast cell exocytosis. It also inhibits Mg-dependent PAP. These in vitro activities confirm its profile as a potent and selective iPLA2 inhibitor. Its effects on iPLA2 activity and mast cell function have been demonstrated in various assays. |
| ln Vivo |
In vivo, BEL is used as a research tool to study the role of iPLA2 in various physiological and pathological processes. However, specific details of in vivo efficacy studies are not extensively detailed in the available literature. The compound is primarily used in in vitro and ex vivo research settings. Its in vivo effects are related to its inhibition of iPLA2.
|
| Enzyme Assay |
The in vitro enzyme assay for BEL measures its ability to inhibit iPLA2 activity. These cell-free assays use purified iPLA2 and a substrate such as arachidonoyl-thio-PC. The compound's inhibitory potency (IC50) is determined by measuring the reduction in enzyme activity. BEL shows an IC50 of approximately 7 μM for iPLA2β.
|
| Cell Assay |
In vitro cellular assays for BEL assess its effects on iPLA2-mediated cellular functions. Mast cells are treated with BEL, and antigen-stimulated exocytosis is measured. Other cell types can be used to assess the effects of iPLA2 inhibition on various cellular processes such as proliferation, apoptosis, and lipid metabolism.
|
| Animal Protocol |
In vivo animal studies for BEL are conducted to assess the role of iPLA2 in various disease models. However, specific details of these studies are not extensively detailed in the available literature. The compound is primarily used as a research tool in cell-based and biochemical studies. Its in vivo pharmacokinetics and toxicity are not well-characterized.
|
| ADME/Pharmacokinetics |
Specific pharmacokinetic data for BEL are not extensively detailed in the available literature. As a research compound, its pharmacokinetic properties such as absorption, distribution, metabolism, and excretion are not well-characterized. The compound is primarily used in in vitro research settings. Its pharmacokinetic profile would be important for its development as a therapeutic agent.
|
| Toxicity/Toxicokinetics |
Specific toxicity data for BEL are not extensively detailed in the available literature. As an irreversible inhibitor of iPLA2, its toxicity profile is likely related to its mechanism of action. However, preclinical toxicology studies would be required to assess its safety margin. The compound is intended for research use only and is not for human use.
|
| References |
|
| Additional Infomation |
Bromoenol lactone is a type of naphthalene compound.
BEL (Bromoenol lactone) is an irreversible, potent, and selective inhibitor of calcium-independent phospholipase A2 (iPLA2β) with an IC50 of approximately 7 μM. It is also known as HELSS. BEL inhibits antigen-stimulated mast cell exocytosis. It is a research compound used for studying the role of iPLA2 in various physiological and pathological processes. It is not approved for clinical use. |
| Molecular Formula |
C16H13O2BR
|
|---|---|
| Molecular Weight |
317.17722
|
| Exact Mass |
316.009
|
| CAS # |
88070-98-8
|
| Related CAS # |
(S)-Bromoenol lactone;478288-94-7;(R)-Bromoenol lactone;478288-90-3;(S)-Bromoenol lactone-d7
|
| PubChem CID |
5940264
|
| Appearance |
White to yellow solid powder
|
| Density |
1.5±0.1 g/cm3
|
| Boiling Point |
467.0±45.0 °C at 760 mmHg
|
| Flash Point |
236.2±28.7 °C
|
| Vapour Pressure |
0.0±1.2 mmHg at 25°C
|
| Index of Refraction |
1.716
|
| LogP |
4.36
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
1
|
| Heavy Atom Count |
19
|
| Complexity |
377
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C1C/C(=C\Br)/OC(=O)C1C2=CC=CC3=CC=CC=C32
|
| InChi Key |
BYUCSFWXCMTYOI-ZRDIBKRKSA-N
|
| InChi Code |
InChI=1S/C16H13BrO2/c17-10-12-8-9-15(16(18)19-12)14-7-3-5-11-4-1-2-6-13(11)14/h1-7,10,15H,8-9H2/b12-10+
|
| Chemical Name |
(6E)-6-(bromomethylidene)-3-naphthalen-1-yloxan-2-one
|
| 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) |
DMSO : ~50 mg/mL (~157.64 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (7.88 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (7.88 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.88 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1528 mL | 15.7639 mL | 31.5278 mL | |
| 5 mM | 0.6306 mL | 3.1528 mL | 6.3056 mL | |
| 10 mM | 0.3153 mL | 1.5764 mL | 3.1528 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03256331 | Terminated | Drug: BEL-X-HG | Advanced Solid Tumors | Belx Bio-Pharmaceutical (Taiwan) Corporation | 2017-06-21 | Phase 1 |
| NCT02619318 | Completed | Behavioral: Balancing Everyday Life (BEL) Behavioral: Care as usual (generally standard occupational therapy) |
Major Psychiatric Disorder | Lund University | 2013-11 | Not Applicable |
| NCT04784039 | Not yet recruiting | Diagnostic Test: Transesophageal echocardiography Diagnostic Test: D-Dimer analysis |
Atrial Fibrillation | AZ Sint-Jan AV | 2025-01-01 | Phase 4 |
| NCT00500903 | Completed | Drug: Alisertib | Advanced Malignancies | Millennium Pharmaceuticals, Inc. | 2007-05-15 | Phase 1 |
| NCT01055795 | Completed | Drug: Bevacizumab, Everolimus and LBH589 | Advanced Solid Tumors | Herbert Hurwitz | 2010-03 | Phase 1 |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA