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Anti-inflammatory agent 47 2925288-12-4

Anti-inflammatory agent 47 2925288-12-4

CAS No.: 2925288-12-4

Flo8 is a potent anti-inflammatory and antioxidant compound. Flo8 can inhibit the release of intracellular reactive oxyg
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Flo8 is a potent anti-inflammatory and antioxidant compound. Flo8 can inhibit the release of intracellular reactive oxygen species (ROS) and nitric oxide (NO), and inhibit neuronal apoptosis by inhibiting inflammation and apoptosis signaling pathways, and may be utilized in the study of PD/Parkinson's disease.

Physicochemical Properties


CAS # 2925288-12-4
Appearance Typically exists as solid at room temperature
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)

Biological Activity


ln Vitro Compound Flo8 exhibits a slight negative effect on BV2 cell viability at 5 μM, 10 μM, and 18 hours [1]. In BV2 cells, compound Flo8 (5 μM, 18 hours) significantly inhibits the generation of ROS [1]. Compound Flo8 (5 μM, 10 μM, 18 hours) inhibits the expression of inflammatory factors in BV2 cells, which lowers the amount of apoptosis in SH-SY5Y cells [1]. Compound Flo8 (5 μM, 10 μM, 18 hours) enhances M2 polarization and prevents LPS-induced M1 polarization in microglia [1]. In BV2 cells, compound Flo8 (5 μM, 10 μM, 18 hours) suppresses phosphorylation of ERK, p38, and JNK caused by LPS [1].
ln Vivo In the brains of C57BL/6J mice, compound Flo8 (15/35 mg/kg, intraperitoneal injection, daily/two weeks) can reduce MPTP-induced neuroinflammation and prevent neuroapoptosis [1].
Cell Assay Cell Cytotoxicity Assay[1]
Cell Types: BV2 cells
Tested Concentrations: 5 μM, 10 μM
Incubation Duration: 18 h
Experimental Results: demonstrated low cytotoxicity at 5 μM concentration and demonstrated minimal toxicity at 10 μM for BV2 cells.

Real Time qPCR[1]
Cell Types: BV2 cells
Tested Concentrations: 5 μM, 10 μM
Incubation Duration: 18 h
Experimental Results: Suppressed LPS-induced expression of M1 markers and increased the mRNA level of CD206, Arg-1, and IL-10 in BV2 cells. diminished the mRNA expression levels of apoptosis-related genes BAX, Caspase3 and Cleaved Caspase3 but increased the expression levels of Bcl-2 in SH-SY5Y cells.

Western Blot Analysis[1]
Cell Types: BV2 cells
Tested Concentrations: 5 μM, 10 μM
Incubation Duration: 18 h
Experimental Results: Inhibited phosphorylation of ERK, p38 and JNK in BV2 cells. Inhibited LPS-induced expression of p-Iκ B- α, p-NF-κB in BV2 cells. diminished the protein expression levels of apoptosis-related genes BAX, Caspase3 and Cleaved Caspase3 but increased the expression levels of Bcl-2 in SH-SY5Y cells.

Immunofluorescence[1]
Animal Protocol Animal/Disease Models: MPTP C57BL/6J mice model[1]
Doses: 15 mg/kg, 35 mg/kg
Route of Administration: intraperitoneal (ip)injection
Experimental Results: Increased the mRNA expression of CD86, TNF-α, IL-6 and IL-1β but diminished CD206, Arg-1 and IL-10 in brain tissue. Inhibited the expression of MPTP-induced phosphorylation of p38, ERK, JNK and NF-κ B. diminished dopamine levels in mouse serum in the MPTP group. Increased the protein expression of Caspase3 and BAX but diminished the expression of Bcl2 after MPTP induction in brain tissue.
References

[1]. Design, synthesis, and SAR study of novel flavone 1,2,4-oxadiazole derivatives with anti-inflammatory activities for the treatment of Parkinson's disease. Eur J Med Chem. 2023 Jul 5;255:115417.


Solubility Data


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
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution 50 μL Tween 80 850 μL Saline)
*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).
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)]
*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.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO 100 μLPEG300 200 μL castor oil 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300:Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH 400 μLPEG300 50 μL Tween 80 450 μL 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).
Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (Please use freshly prepared in vivo formulations for optimal results.)