BF-168 is a candidate probe for PET that can specifically identify neural and diffuse plaques with Ki of 6.4 nM for Aβ1-42.

Physicochemical Properties

Molecular Formula	C18H17FN2O2
Molecular Weight	312.338187932968
Exact Mass	312.127
CAS #	634911-47-0
PubChem CID	10244995
Appearance	White to yellow solid powder
LogP	4.4
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	5
Rotatable Bond Count	6
Heavy Atom Count	23
Complexity	385
Defined Atom Stereocenter Count	0
SMILES	FCCOC1C=CC2=C(C=1)OC(/C=C/C1C=CC(=CC=1)NC)=N2
InChi Key	FJCPWUDGNYOGQR-RUDMXATFSA-N
InChi Code	InChI=1S/C18H17FN2O2/c1-20-14-5-2-13(3-6-14)4-9-18-21-16-8-7-15(22-11-10-19)12-17(16)23-18/h2-9,12,20H,10-11H2,1H3/b9-4+
Chemical Name	4-[(E)-2-[6-(2-fluoroethoxy)-1,3-benzoxazol-2-yl]ethenyl]-N-methylaniline
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 Note: This product is not stable in solution, please use freshly prepared working solution for optimal results.
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	Styrylbenzoxazole derivative BF-168 is a powerful medication that specifically identifies SP and NFT in AD brains. BF-168 is a potential PET probe that has been shown to distinguish between neuritic and diffuse plaques with a 6.4 nM Ki value of Aβ1-42 [1].
ln Vivo	In APP23 and PS1/APP transgenic mice, intravenous injection of BF-168 led to precise in vivo labeling of diffuse and dense amyloid plaques in the brain. Additionally, in normal mice, 18F radiolabeled BF-168 demonstrated quick clearance (t1/2 = 24.7 min) and substantial initial brain uptake (3.9% of injected dose/g 2 min after injection). Additionally, 180 minutes following intravenous injection of [18F]BF-168, brain slices from APP23 transgenic mice were autoradiographically labeled selectively for brain amyloid plaques with minimal non-specific binding [1].
References	[1]. Styrylbenzoxazole derivatives for in vivo imaging of amyloid plaques in the brain. J Neurosci. 2004 Mar 10;24(10):2535-41.

Solubility Data

Solubility (In Vitro)

DMSO : ~50 mg/mL (~160.08 mM)

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	3.2016 mL	16.0082 mL	32.0164 mL
	5 mM	0.6403 mL	3.2016 mL	6.4033 mL
	10 mM	0.3202 mL	1.6008 mL	3.2016 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.