| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 50mg | |||
| Other Sizes |
| Targets |
Bisabolangelone primarily targets the NF-kappaB and MAPK signaling pathways. It inhibits LPS-stimulated inflammation in macrophages by blocking the activation of these pathways. At the molecular level, Bisabolangelone inhibits MAPK phosphorylation and prevents the nuclear translocation of NF-kappaB p50/p65. By blocking MAPK and NF-kappaB signaling, the compound inhibits the function of dendritic cells, reducing the production of pro-inflammatory cytokines including interleukin (IL)-12, IL-1beta, and tumor necrosis factor-alpha (TNF-alpha). It also inhibits migration to macrophage inflammatory protein-3 beta and reduces the ability of dendritic cells to activate allogeneic T cells.
|
|---|---|
| ln Vitro |
In vitro, Bisabolangelone (BISA) exhibits anti-inflammatory activity by reducing the production of pro-inflammatory cytokines including IL-12, IL-1beta, and TNF-alpha in dendritic cells. It inhibits LPS-stimulated inflammation in macrophages by blocking the NF-kappaB and MAPK pathways. The compound also inhibits dendritic cell functions, including migration to macrophage inflammatory protein-3 beta and the ability to activate allogeneic T cells. Molecular studies have shown that Bisabolangelone inhibits MAPK phosphorylation and prevents the nuclear translocation of NF-kappaB p50/p65. Additionally, it exhibits anti-tumor, anti-microbial, and antioxidant activities in various in vitro systems.
|
| ln Vivo |
In vivo, Bisabolangelone has demonstrated anti-inflammatory and anti-ulcer activities. Its anti-inflammatory effects are mediated through the blockade of NF-kappaB and MAPK pathways, leading to reduced production of pro-inflammatory cytokines. The compound has been studied for its potential in treating inflammation-related conditions and ulcer diseases. Its anti-tumor and antimicrobial activities observed in vitro suggest potential applications in cancer and infection-related studies. Further in vivo studies are needed to fully characterize its efficacy, pharmacokinetics, and safety profile in animal models of these diseases.
|
| Enzyme Assay |
Cell-free assays for Bisabolangelone typically involve assessing its inhibition of NF-kappaB and MAPK signaling. For NF-kappaB inhibition, a cell-free electrophoretic mobility shift assay (EMSA) can be used, where nuclear extracts are incubated with a radiolabeled NF-kappaB consensus oligonucleotide probe in the presence or absence of Bisabolangelone. The DNA-protein complexes are resolved on a non-denaturing polyacrylamide gel and visualized by autoradiography. For MAPK inhibition, recombinant MAPK enzymes (e.g., p38, JNK, ERK) are incubated with a peptide substrate, ATP, and various concentrations of Bisabolangelone in a kinase buffer. The phosphorylation of the substrate is measured using a kinase activity assay kit.
|
| Cell Assay |
For in vitro cellular experiments, macrophages or dendritic cells are cultured in appropriate media and treated with Bisabolangelone at various concentrations (typically 1-100 uM). Cells are stimulated with LPS in the presence or absence of the compound, and the production of pro-inflammatory cytokines (IL-12, IL-1beta, TNF-alpha) is measured by ELISA or qRT-PCR. NF-kappaB activation is assessed by measuring the nuclear translocation of p50/p65 using immunofluorescence or Western blot. MAPK phosphorylation is assessed by Western blot using phospho-specific antibodies. The duration of treatment varies depending on the experimental design but typically ranges from 6 to 24 hours.
|
| Animal Protocol |
In vivo animal experiments with Bisabolangelone typically involve oral or intraperitoneal administration in rodent models of inflammation or ulcer. A common dosing regimen is 10-50 mg/kg body weight, administered daily for 1-4 weeks. For anti-inflammatory studies, animals are treated with Bisabolangelone before or after induction of inflammation (e.g., by LPS injection or carrageenan-induced paw edema), and inflammatory markers are measured in blood and tissue samples. For anti-ulcer studies, animals are treated with the compound before induction of gastric ulcers (e.g., by ethanol or indomethacin), and the ulcer index is assessed by histological examination. Blood and tissue samples are collected for biochemical analysis.
|
| ADME/Pharmacokinetics |
Bisabolangelone has a molecular weight of 248.32 g/mol and a molecular formula of C15H20O3. It is soluble in DMSO (25 mg/mL) and has a density of 1.154 g/cm3. For in vivo studies, it can be formulated in 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% saline at a concentration of 2 mg/mL. The compound is stable as a powder at -20degC for up to 3 years and in solution at -80degC for 1 year. Further pharmacokinetic studies are needed to characterize its absorption, distribution, metabolism, and excretion properties.
|
| Toxicity/Toxicokinetics |
The toxicity profile of Bisabolangelone has not been extensively characterized. As a natural product with anti-inflammatory and anti-tumor activities, it is expected to have a favorable safety profile at pharmacological doses. However, the compound's ability to inhibit NF-kappaB and MAPK pathways, which are involved in immune responses and cell survival, may have potential toxicities at higher doses. The compound should be handled with standard laboratory precautions and is intended for research use only. Further toxicological studies are needed to establish its full safety profile.
|
| References |
|
| Additional Infomation |
Bisapologide has been reported to be found in Angelica biserrata, Ostericum grosseserratum, and Angelica pubescens, and relevant data are available for reference.
Bisabolangelone is a sesquiterpene derivative isolated from the roots of Osterici Radix (Angelica species). It possesses anti-tumor, anti-inflammatory, anti-microbial, and antioxidant activities. The compound inhibits LPS-stimulated inflammation by blocking the NF-kappaB and MAPK pathways in macrophages. It also exhibits anti-ulcer activities and inhibits dendritic cell functions by blocking MAPK and NF-kappaB signaling. Bisabolangelone has potential applications in cancer, infection, and inflammation-related research. It is available as a research compound and is not approved for clinical use. |
| Molecular Formula |
C15H20O3
|
|---|---|
| Molecular Weight |
248.317504882813
|
| Exact Mass |
248.141
|
| CAS # |
30557-81-4
|
| PubChem CID |
12300142
|
| Appearance |
Off-white to yellow solid powder
|
| LogP |
2.521
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
1
|
| Heavy Atom Count |
18
|
| Complexity |
466
|
| Defined Atom Stereocenter Count |
3
|
| SMILES |
CC1=CC(=O)[C@H]2[C@@H](C1)O/C(=C\C=C(C)C)/[C@@]2(C)O
|
| InChi Key |
GNWNPLBSEQDDQV-FRPWFYLFSA-N
|
| InChi Code |
InChI=1S/C15H20O3/c1-9(2)5-6-13-15(4,17)14-11(16)7-10(3)8-12(14)18-13/h5-7,12,14,17H,8H2,1-4H3/b13-6-/t12-,14+,15-/m1/s1
|
| Chemical Name |
(2Z,3S,3aS,7aR)-3-hydroxy-3,6-dimethyl-2-(3-methylbut-2-enylidene)-7,7a-dihydro-3aH-1-benzofuran-4-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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : ~100 mg/mL (~402.71 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.07 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
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 (10.07 mM) (saturation unknown) 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. 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 (10.07 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 | 4.0271 mL | 20.1353 mL | 40.2706 mL | |
| 5 mM | 0.8054 mL | 4.0271 mL | 8.0541 mL | |
| 10 mM | 0.4027 mL | 2.0135 mL | 4.0271 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
