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Nrf2/HO-1 activator 1 2883506-60-1

Nrf2/HO-1 activator 1 2883506-60-1

CAS No.: 2883506-60-1

Nrf2/HO-1 activator 1 (Compound 24) is a potent Nrf2/HO-1 activator and neuro-protection agent. Nrf2/HO-1 activator 1 ha
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This product is for research use only, not for human use. We do not sell to patients.

Nrf2/HO-1 activator 1 (Compound 24) is a potent Nrf2/HO-1 activator and neuro-protection agent. Nrf2/HO-1 activator 1 has neuro-protection and antioxidant activities. Nrf2/HO-1 activator 1 may be utilized in PD/Parkinson's disease research.

Physicochemical Properties


Molecular Formula C21H18O5
Molecular Weight 350.36
CAS # 2883506-60-1
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 Nrf2/HO-1 activator 1 (0.3-30 µM; 24 h) displays effective neuroprotection in both 6-OHDA- and rotenone-induced cell death models[1]. Nrf2/HO-1 activator 1 (1-30 µM; 6 h) enhances HO-1 expression in PC12 cells[1]. Nrf2/HO-1 activator 1 (12 µM; 1-12 h) enhances phosphorylation of ERK1/2, JNK, and Akt in PC12 cells[1].
ln Vivo Rat brain homogenates' ability to produce lipid peroxide is 50.5% inhibited by Nrf2/HO-1 activator 1 at 100 μM[1].
Cell Assay Cell Viability Assay[1]
Cell Types: PC12 cells
Tested Concentrations: 0.3, 1, 3, 10, and 30 μM
Incubation Duration: 4 hrs (hours)
Experimental Results: Inhibited 6-OHDA-induced toxicity with IC50 of 3.9 μM. Inhibited rotenone-induced toxicity with IC50 of 4.8 μM.

Western Blot Analysis[1]
Cell Types: PC12 cells
Tested Concentrations: 10 μM
Incubation Duration: 1, 3, 6, and 12 hrs (hours)
Experimental Results: Induced phosphorylation of ERK1/2, JNK, and Akt.

Western Blot Analysis[1]
Cell Types: PC12 cells
Tested Concentrations: 1, 3, 10, and 30 μM
Incubation Duration: 6 hrs (hours)
Experimental Results: Increased HO-1 expression in a dose-dependent manner, with 2-fold increases at 30 μM concentrations.
References

[1]. Novel cudraisoflavone J derivatives as potent neuroprotective agents for the treatment of Parkinson's disease via the activation of Nrf2/HO-1 signaling. Eur J Med Chem. 2022 Nov 15;242:114692.


Solubility Data


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.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.8542 mL 14.2710 mL 28.5421 mL
5 mM 0.5708 mL 2.8542 mL 5.7084 mL
10 mM 0.2854 mL 1.4271 mL 2.8542 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.