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.

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)

Biological Activity

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.

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.)

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.