DFB

Allosteric potentiator at mGlu5 CAS# 15332-10-2

DFB

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Chemical structure

DFB

3D structure

Chemical Properties of DFB

Cas No. 15332-10-2 SDF Download SDF
PubChem ID 5678496 Appearance Powder
Formula C14H10F2N2 M.Wt 244.24
Type of Compound N/A Storage Desiccate at -20°C
Synonyms 3,3'-Difluorobenzaldazine
Solubility Soluble to 10 mM in ethanol and to 50 mM in DMSO
Chemical Name (Z)-1-(3-fluorophenyl)-N-[(Z)-(3-fluorophenyl)methylideneamino]methanimine
SMILES C1=CC(=CC(=C1)F)C=NN=CC2=CC(=CC=C2)F
Standard InChIKey YYMCVDNIIFNDJK-XFQWXJFMSA-N
Standard InChI InChI=1S/C14H10F2N2/c15-13-5-1-3-11(7-13)9-17-18-10-12-4-2-6-14(16)8-12/h1-10H/b17-9-,18-10-
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of DFB

DescriptionNovel allosteric potentiator of the metabotropic glutamate receptor mGlu5. Devoid of agonist activity itself, but potentiates (3 - 6-fold) the action of agonists at mGlu5 without any effect at other mGlu subtypes (EC50 for potentiation = 2 - 5.3 μM).

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DFB Molarity Calculator

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Preparing Stock Solutions of DFB

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 4.0943 mL 20.4717 mL 40.9433 mL 81.8867 mL 102.3583 mL
5 mM 0.8189 mL 4.0943 mL 8.1887 mL 16.3773 mL 20.4717 mL
10 mM 0.4094 mL 2.0472 mL 4.0943 mL 8.1887 mL 10.2358 mL
50 mM 0.0819 mL 0.4094 mL 0.8189 mL 1.6377 mL 2.0472 mL
100 mM 0.0409 mL 0.2047 mL 0.4094 mL 0.8189 mL 1.0236 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on DFB

Room Temperature O-band DFB Laser Array Directly Grown on (001) Silicon.[Pubmed:27997215]

Nano Lett. 2017 Jan 11;17(1):559-564.

Several approaches for growing III-V lasers on silicon were recently demonstrated. Most are not compatible with further integration, however, and rely on thick buffer layers and require special substrates. Recently, we demonstrated a novel approach for growing high quality InP without buffer on standard 001-silicon substrates using a selective growth process compatible with integration. Here we show high quality InGaAs layers can be grown on these InP-templates. High-resolution TEM analysis shows these layers are free of optically active defects. Contrary to InP, the InGaAs material exhibits strong photoluminescence for wavelengths relevant for integration with silicon photonics integrated circuits. Distributed feedback lasers were defined by etching a first order grating in the top surface of the device. Clear laser operation at a single wavelength with strong suppression of side modes was demonstrated. Compared to the previously demonstrated InP lasers 65% threshold reduction is observed. Demonstration of laser arrays with linearly increasing wavelength prove the control of the process and the high quality of the material. This is an important result toward realizing fully integrated photonic ICs on silicon substrates.

First demonstration and field trial on multi-user UDWDM-PON full duplex PSK-PSK with single monolithic integrated dual-output-DFB-SOA based ONUs.[Pubmed:28005870]

Opt Lett. 2016 Oct 15;41(20):4696-4699.

We demonstrate a monolithically integrated dual-output DFB-SOA, and conduct the field trial on a multi-user bidirectional coherent ultradense wavelength division multiplexing-passive optical network (UDWDM-PON). To the best of our knowledge, this is the first achievement of simplified single integrated laser-based neighboring coherent optical network units (ONUs) with a 12.5 GHz channel spaced ultra-dense access network, including both downstream and upstream, taking the benefits of low footprint and low-temperature dependence.

Chirp evaluation of semiconductor DFB lasers through a simple Interferometry-Based (IB) technique.[Pubmed:27828008]

Appl Opt. 2016 Oct 1;55(28):7788-7795.

Direct modulation of a laser source is often utilized in realizing optical fiber connections where the cost of the entire system must be kept at a low level. An undesired consequence of this choice is the onset of the laser frequency chirp effect, which is detrimental in the case of either digital or analog links, and must be evaluated with precision in order to perform an accurate design of the whole system. Various methods of evaluation of the chirp parameters have been proposed, and the choice among them is typically made on the basis of the laboratory equipment available at the moment. This paper adds a further element to the set of possible choices, since it presents a method for the evaluation of the adiabatic chirp factor in distributed feedback (DFB) laser sources, which exploits a simple interferometric scheme, guarantees low cost, and shows, at the same time, good accuracy of the results.

1.3-mum dual-wavelength DFB laser chip with modulation bandwidth enhancement by integrated passive optical feedback.[Pubmed:27958552]

Opt Express. 2016 Dec 12;24(25):28869-28876.

We report a 1.3-mum dual-wavelength distributed feedback (DFB) photonic integrated chip with modulation bandwidth enhancement using integrated optical feedback section. The dual-wavelength DFB lasers were realized using the upper separate confinement heterostructure (SCH) selective area growth (SAG) approach. A modified butt-joint technique was also adopted to achieve high-quality active-passive interface and minimize unintentional intra-cavity optical feedbacks. The fabricated photonic chip exhibited stable single mode operations with a wavelength separation of 2.06 nm. The 3-dB modulation bandwidth was enhanced through the photon-photon resonance effect with f3dB > 17 GHz and open eyes up to 25 Gbit/s for both channels were also obtained. The design can also be scaled up to higher channel counts and higher data rate.

Allosteric potentiators of metabotropic glutamate receptor subtype 5 have differential effects on different signaling pathways in cortical astrocytes.[Pubmed:16135701]

J Pharmacol Exp Ther. 2005 Dec;315(3):1212-9.

The metabotropic glutamate receptor subtype 5 (mGluR5) activates calcium mobilization and extracellular signal-regulated kinase 1/2 (ERK1/2) phosphorylation in cortical astrocytes. These are independent signaling systems, and they can be differentially regulated. We recently discovered two novel selective allosteric potentiators of mGluR5, 3,3'-difluorobenzaldazine (DFB) and N-{4-chloro-2-[(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl) methyl]phenyl}-2-hydroxybenzamide (CPPHA). In studies of mGluR5 activation of calcium transients in recombinant systems, both DFB and CPPHA are without effect on baseline calcium levels, but they induce parallel leftward shifts in the concentration-response curve to agonists. However, it is conceivable that these compounds will have differential effects on different signaling pathways in native systems. Here, we examined the effects of CPPHA and DFB on mGluR5-induced calcium transients and ERK1/2 phosphorylation in cultured rat cortical astrocytes. Both potentiators induced parallel leftward shifts of the concentration-response curves of DHPG- and glutamate-induced calcium transients in astrocytes. These effects are identical to their effects on mGluR5 expressed in human embryonic kidney 293 or Chinese hamster ovary cells. DFB induced a similar shift of concentration-response curve of DHPG-induced ERK1/2 phosphorylation. Interestingly, CPPHA induced an increase in basal mGluR5-mediated ERK1/2 phosphorylation and potentiated the effect of low concentrations of agonists. In contrast, CPPHA significantly decreased ERK1/2 phosphorylation induced by high concentrations of agonists. Thus, CPPHA has qualitatively different effects on mGluR5-mediated calcium responses and ERK1/2 phosphorylation. Together, these data provide evidence that different allosteric potentiators can differentially modulate coupling of a single receptor to different signaling pathways.

A family of highly selective allosteric modulators of the metabotropic glutamate receptor subtype 5.[Pubmed:12920211]

Mol Pharmacol. 2003 Sep;64(3):731-40.

We have identified a family of highly selective allosteric modulators of the group I metabotropic glutamate receptor subtype 5 (mGluR5). This family of closely related analogs exerts a spectrum of effects, ranging from positive to negative allosteric modulation, and includes compounds that do not themselves modulate mGluR5 agonist activity but rather prevent other family members from exerting their modulatory effects. 3,3'-Difluorobenzaldazine (DFB) has no agonist activity, but it acts as a selective positive allosteric modulator of human and rat mGluR5. DFB potentiates threshold responses to glutamate, quisqualate, and 3,5-dihydroxyphenylglycine in fluorometric Ca2+ assays 3- to 6-fold, with EC50 values in the 2 to 5 microM range, and at 10 to 100 microM, it shifts mGluR5 agonist concentration-response curves approximately 2-fold to the left. The analog 3,3'-dimethoxybenzaldazine (DMeOB) acts as a negative modulator of mGluR5 agonist activity, with an IC50 of 3 microM in fluorometric Ca2+ assays, whereas the analog 3,3'-dichlorobenzaldazine (DCB) does not exert any apparent modulatory effect on mGluR5 activity. However, DCB seems to act as an allosteric ligand with neutral cooperativity, preventing the positive allosteric modulation of mGluRs by DFB as well as the negative modulatory effect of DMeOB. None of these analogs affects binding of [3H]quisqualate to the orthosteric (glutamate) site, but they do inhibit [3H]3-methoxy-5-(2-pyridinylethynyl)pyridine binding to the site for 2-methyl-6-(phenylethynyl)-pyridine, a previously identified negative allosteric modulator. With the use of these compounds, we provide evidence that allosteric sites on GPCRs can respond to closely related ligands with a range of pharmacological activities from positive to negative modulation as well as to neutral competition of this modulation.

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