| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| Other Sizes |
| Targets |
Grossamide possesses potential anti-inflammatory effects and has potential anti-neuroinflammatory effects against lipopolysaccharide (LPS)-induced inflammatory response in BV2 microglia cells. It may target inflammatory pathways such as TLR-4-mediated NF-κB signaling.
|
|---|---|
| ln Vitro |
LPS-mediated inflammatory molecule synthesis is downregulated by grossamide [1]. In a dose-dependent way, grossamide (0-20 μM, 1 hour) suppresses TNF-α and IL-6 mRNA levels, NF-κB activation produced by LPS, and LPS-induced TLR4 and MyD88 expression without causing cytotoxicity. ..1].
In vitro, Grossamide has been shown to possess potential anti-inflammatory effects. It has potential anti-neuroinflammatory effects against LPS-induced inflammatory response in BV2 microglia cells. It suppresses TLR-4-mediated NF-κB signaling pathways in LPS-stimulated BV2 microglia cells. It reduces TNF-α and IL-6 in a dose-dependent manner. |
| ln Vivo |
In vivo data for Grossamide are limited in the available literature. As a natural product with anti-inflammatory properties, it may have potential for research in neuroinflammation and related conditions. Further in vivo studies are needed to evaluate its therapeutic potential.
|
| Enzyme Assay |
Grossamide's anti-neuroinflammatory activity can be characterized in BV2 microglia cells. Cells are stimulated with LPS to induce an inflammatory response, and Grossamide is tested for its ability to suppress inflammatory markers such as TNF-α and IL-6. Its effects on TLR-4-mediated NF-κB signaling pathways can be assessed.
|
| Cell Assay |
RT-PCR[1]
Cell Types: BV-2 Microglia Tested Concentrations: 0, 10, 15 and 20 μM Incubation Duration: 1 hour and co-culture with LPS (100 ng/mL) for another 6 hrs (hours) Experimental Results: Inhibition of TNF- α and IL-6 mRNA levels were dose-dependent. Western Blot Analysis[1] Cell Types: BV-2 Microglia Tested Concentrations: 0, 10, 15 and 20 μM Incubation Duration: 1 hour followed by stimulation with LPS (100 ng/mL) for 1 hour or 24 hrs (hours) Experimental Results: LPS Inhibited - phosphorylation that induces IκBα phosphorylation and Dramatically reduces NF-κB p65 levels. The expression of TLR4 and MyD88 diminished in a dose-dependent manner. Cell viability assay[1] Cell Types: BV-2 Microglia Tested Concentrations: 0, 10, 15 and 20 μM Incubation Duration: 1 hour, 24 hour co-culture in the absence or presence of 100 ng/mL LPS Experimental Results: No cytotoxicity. In vitro cell experiments with Grossamide use BV2 microglia cells. Cells are pretreated with Grossamide at concentrations of 10, 15, and 20 μM, followed by LPS stimulation. The compound's effects on TNF-α and IL-6 production are measured in a dose-dependent manner. |
| Animal Protocol |
In vivo animal studies with Grossamide have not been extensively reported in the available literature. The compound is a natural product from Cannabis sativa and Polygonum species. Further studies are needed to evaluate its in vivo efficacy and safety in animal models of neuroinflammation.
|
| ADME/Pharmacokinetics |
Pharmacokinetic data for Grossamide are not available in the searched literature. As a natural product with a molecular weight of 624.68, the compound may have limited oral bioavailability. Further pharmacokinetic studies are needed to characterize its absorption, distribution, metabolism, and excretion properties.
|
| Toxicity/Toxicokinetics |
Grossamide is considered safe for research use at typical concentrations. As a natural product, it is generally considered to have a favorable safety profile. As a research compound, it is intended for laboratory use only and not for human consumption.
|
| References |
[1]. Luo Q, et al. Anti-neuroinflammatory effects of grossamide from hemp seed via suppression of TLR-4-mediated NF-κB signaling pathways in lipopolysaccharide-stimulated BV2 microglia cells. Mol Cell Biochem. 2017 Apr;428(1-2):129-137.
|
| Additional Infomation |
Macrolides have been reported to be present in chili peppers (Capsicum annuum), and relevant data are available.
See also: Macrolides (note moved to). Grossamide (GSE) is a lignanamide from Polygonum species with potential anti-inflammatory and anti-neuroinflammatory effects. It suppresses TLR-4-mediated NF-κB signaling pathways in LPS-stimulated BV2 microglia cells. It has a molecular formula of C₃₆H₃₆N₂O₈ and a molecular weight of 624.68. |
| Molecular Formula |
C36H36N2O8
|
|---|---|
| Molecular Weight |
624.6797
|
| Exact Mass |
624.247
|
| CAS # |
80510-06-1
|
| PubChem CID |
5322012
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.3±0.1 g/cm3
|
| Boiling Point |
934.8±65.0 °C at 760 mmHg
|
| Melting Point |
174 - 175 °C
|
| Flash Point |
519.2±34.3 °C
|
| Vapour Pressure |
0.0±0.3 mmHg at 25°C
|
| Index of Refraction |
1.654
|
| LogP |
2.98
|
| Hydrogen Bond Donor Count |
5
|
| Hydrogen Bond Acceptor Count |
8
|
| Rotatable Bond Count |
12
|
| Heavy Atom Count |
46
|
| Complexity |
995
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C([C@@H]1[C@@H](C2C=CC(O)=C(OC)C=2)OC2C(=CC(=CC1=2)/C=C/C(=O)NCCC1C=CC(O)=CC=1)OC)(=O)NCCC1C=CC(O)=CC=1
|
| InChi Key |
DROXVBRNXCRUHP-VGOFMYFVSA-N
|
| InChi Code |
InChI=1S/C36H36N2O8/c1-44-30-21-25(8-13-29(30)41)34-33(36(43)38-18-16-23-5-11-27(40)12-6-23)28-19-24(20-31(45-2)35(28)46-34)7-14-32(42)37-17-15-22-3-9-26(39)10-4-22/h3-14,19-21,33-34,39-41H,15-18H2,1-2H3,(H,37,42)(H,38,43)/b14-7+
|
| Chemical Name |
2-(4-hydroxy-3-methoxyphenyl)-N-[2-(4-hydroxyphenyl)ethyl]-5-[(E)-3-[2-(4-hydroxyphenyl)ethylamino]-3-oxoprop-1-enyl]-7-methoxy-2,3-dihydro-1-benzofuran-3-carboxamide
|
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| 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 | 1.6008 mL | 8.0041 mL | 16.0082 mL | |
| 5 mM | 0.3202 mL | 1.6008 mL | 3.2016 mL | |
| 10 mM | 0.1601 mL | 0.8004 mL | 1.6008 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
