PeptideDB

Akt/NF-κB/MAPK-IN-1

Akt/NF-κB/MAPK-IN-1

CAS No.:

Akt/NF-κB/MAPK-IN-1 (compound 2m) is an orally bioactive NO inhibitor (IC50=7.70 μM) without obvious toxicity. Akt/NF-
Sales Email:peptidedb@qq.com

This product is for research use only, not for human use. We do not sell to patients.

Akt/NF-κB/MAPK-IN-1 (compound 2m) is an orally bioactive NO inhibitor (IC50=7.70 μM) without obvious toxicity. Akt/NF-κB/MAPK-IN-1 exerts anti-inflammatory activity by inhibiting the Akt/NF-κB and MAPK signaling pathways.

Physicochemical Properties


Molecular Formula C38H56N2O4
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


Targets IL-1β IL-6 iNOS COX-2
ln Vitro Compound 2m (MAPK-IN-1, Akt/NF-κB) (0–20 μM, 24 hours) can dramatically lower IL-1β and TNF-α in RAW264.LPS (10 ng/mL)-induced levels of IL-6 and PGE2 in 7 cells were seen to downregulate the production of COX-2 and iNOS [1]. RAW264 is resistant to LPS-induced phosphorylation of p38, ERK, and JNK when exposed to Akt/NF-κB/MAPK-IN-1 (0–20 μM, 24 hours).7 cells [1].
ln Vivo Compound 2m, administered intraperitoneally at 10–20 mg/kg for seven days, has been shown to mitigate LPS-induced inflammatory disorders in mice [1].
Animal Protocol Animal/Disease Models: Male ICR mice (weighing 20-25 g)[1]
Doses: 10 and 20 mg/kg
Route of Administration: intragastric (po) administration, for 7 days, and then LPS was intraperitoneally (ip) injected
Experimental Results: The levels of IL-6, IL -1β and TNF-α in the LPS group were Dramatically increased compared to the control group, and the administration of 2m effectively prevented the increase.
References

[1]. Design, synthesis and evaluation of ursodeoxycholic acid-cinnamic acid hybrids as potential anti-inflammatory agents by inhibiting Akt/NF-κB and MAPK signaling pathways. Eur J Med Chem. 2023 Aug 31;260:115785.


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.)