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2'MeO6MF

Cat No.:V71844 Purity: ≥98%
2'MeO6MF is a BBB (blood-brain barrier) permeable (penetrable) PAM (positive allosteric modulator) of α2β1γ2L and all α1-containing GABAA receptors.
2'MeO6MF
2'MeO6MF Chemical Structure CAS No.: 89112-85-6
Product category: GABA Receptor
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
1mg
Other Sizes
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Product Description
2'MeO6MF is a BBB (blood-brain barrier) permeable (penetrable) PAM (positive allosteric modulator) of α2β1γ2L and all α1-containing GABAA receptors. 2'MeO6MF can also directly activate α2β2/3 and α2β2/3γ2L GABAA receptors. 2'MeO6MF has anxiolytic and neuroleptic effects. 2'MeO6MF provides neuroprotection and improves functional recovery and also suppresses stroke-induced inflammatory responses.
Biological Activity I Assay Protocols (From Reference)
Targets
GABAA receptor[1]
ln Vitro
2'MeO6MF (100-300 µM; 60 min) slightly shifts the binding of [3H]-flunitrazepam to the synaptic membranes in rat brain by 5–10%. In a concentration-dependent manner, 2'MeO6MF increases [3H]-muscimol binding to rat brain synaptic membranes, resulting in an apparent EC50=20.8 nM and a mean Emax of 219.8%[1]. At recombinant α1β2γ2L GABAA receptors produced in Xenopus M oocytes, 2'MeO6MF (1-300 µM) concentration-dependently improves the response evoked by a low dose of GABA. Without any direct activation, 2'MeO6MF amplifies the response that GABA elicits at recombinant α1β1,3η2L and α1β2 GABAA receptors[1]. Concentration-dependently, 2'MeO6MF (1-10 µM; 60 min) raises tonic inhibitory currents in granule cells[2]. In RAWblueTM macrophage cells, 2'MeO6MF (100-1000 µM; 6.5 h) suppresses the LPS-induced increase in NFkB activity[2].
ln Vivo
In the elevated plus maze and light/dark tests, 2'MeO6MF (1-100 mg/kg; ip) exhibits anxiolytic-like effects. Higher dosages of MeO6MF produce sedative effects in the holeboard, actimeter, and barbiturate-induced sleep time tests[1]. After a stroke, mice's layer 2/3 pyramidal neurons exhibit an increase in tonic currents when exposed to 30 mg/kg of MeO6MF IV[2]. 2'MeO6MF (0.1-30 mg/kg; ip) protects neurons and improves functional recovery in mice following localized cerebral ischemia[2].
Animal Protocol
Animal/Disease Models: Male Balb-c mice (8-10 weeks, 25-35 g)[1]
Doses: 1, 10, 30, 100 mg/kg
Route of Administration: Ip
Experimental Results: No overt acute toxicity was observed. Exerted anxiolytic effects at low doses and sedative effects at high doses without myorelaxant effects.
References
[1]. Karim N, et, al. 2'-Methoxy-6-methylflavone: a novel anxiolytic and sedative with subtype selective activating and modulating actions at GABA(A) receptors. Br J Pharmacol. 2012 Feb;165(4):880-96.
[2]. Clarkson AN, et, al. The flavonoid, 2'-methoxy-6-methylflavone, affords neuroprotection following focal cerebral ischaemia. J Cereb Blood Flow Metab. 2019 Jul;39(7):1266-1282.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C17H14O3
Molecular Weight
266.29
Exact Mass
266.094
CAS #
89112-85-6
PubChem CID
930492
Appearance
Typically exists as solid at room temperature
LogP
3.777
Hydrogen Bond Donor Count
0
Hydrogen Bond Acceptor Count
3
Rotatable Bond Count
2
Heavy Atom Count
20
Complexity
401
Defined Atom Stereocenter Count
0
SMILES
CC1=CC2=C(C=C1)OC(=CC2=O)C3=CC=CC=C3OC
InChi Key
QEIHFNZSIRWEBX-UHFFFAOYSA-N
InChi Code
InChI=1S/C17H14O3/c1-11-7-8-16-13(9-11)14(18)10-17(20-16)12-5-3-4-6-15(12)19-2/h3-10H,1-2H3
Chemical Name
2-(2-methoxyphenyl)-6-methylchromen-4-one
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 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 : PEG300Tween 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).
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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 : PEG300Tween 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).
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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 3.7553 mL 18.7765 mL 37.5530 mL
5 mM 0.7511 mL 3.7553 mL 7.5106 mL
10 mM 0.3755 mL 1.8777 mL 3.7553 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.

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What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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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