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| 250mg | ||
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| Other Sizes |
| ln Vitro |
4′-Demethylnobiletin (1-100 μM, 0-60 min) can stimulate CRE-mediated transcription by activating the PKA/MEK/ERK-dependent signaling pathway. It can also phosphorylate ERK and CREB in rat hippocampal neurons in a manner that is dependent on time, concentration, and the PKA/MEK/ERK pathway [1].
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| ln Vivo |
4′-Demethylnobiletin (10 or 50 mg/kg, ip, once daily for seven consecutive days) reduced the learning impairment caused by MK-801 in male ddY mice in a dose-dependent manner without impairing the animals's movement. MK-801-treated mice had less freezing than control mice and inhibited the activation of ERK learning in the hippocampal regions of the mice; additionally, 4'-Demethylnobiletin was able to reverse this behavior [1]. For seven days in a row, 4′-Demethylnobiletin (10 or 50 mg/kg, ip, once daily) can reverse the inhibition of MK-801 on phosphorylation of PKA substrate and ERK in response to NMDA stimulation in hippocampal neurons [1].
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| References |
[1]. Md Al Rahim, et al. 4'-Demethylnobiletin, a bioactive metabolite of nobiletin enhancing PKA/ERK/CREB signaling, rescues learning impairment associated with NMDA receptor antagonism via stimulation of the ERK cascade. Biochemistry. 2009 Aug 18;48(32):7713-21.
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| Molecular Formula |
C20H20O8
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|---|---|
| Molecular Weight |
388.37
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| CAS # |
34810-62-3
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| SMILES |
OC1C=CC(C2=CC(=O)C3C(OC)=C(OC)C(OC)=C(OC)C=3O2)=CC=1OC
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| 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.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5749 mL | 12.8743 mL | 25.7486 mL | |
| 5 mM | 0.5150 mL | 2.5749 mL | 5.1497 mL | |
| 10 mM | 0.2575 mL | 1.2874 mL | 2.5749 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.
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