DQP 1105

CAS# 380560-89-4

DQP 1105

Catalog No. BCC6205----Order now to get a substantial discount!

Product Name & Size Price Stock
DQP 1105: 5mg $104 In Stock
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Chemical structure

DQP 1105

3D structure

Chemical Properties of DQP 1105

Cas No. 380560-89-4 SDF Download SDF
PubChem ID 6044308 Appearance Powder
Formula C29H24BrN3O4 M.Wt 558.42
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 100 mM in DMSO
Chemical Name 4-[(3Z)-5-(4-bromophenyl)-3-(6-methyl-2-oxo-4-phenylquinolin-3-ylidene)pyrazolidin-1-yl]-4-oxobutanoic acid
SMILES CC1=CC2=C(C(=C3CC(N(N3)C(=O)CCC(=O)O)C4=CC=C(C=C4)Br)C(=O)N=C2C=C1)C5=CC=CC=C5
Standard InChIKey CADIBCWPGCNUBD-NFFVHWSESA-N
Standard InChI InChI=1S/C29H24BrN3O4/c1-17-7-12-22-21(15-17)27(19-5-3-2-4-6-19)28(29(37)31-22)23-16-24(18-8-10-20(30)11-9-18)33(32-23)25(34)13-14-26(35)36/h2-12,15,24,32H,13-14,16H2,1H3,(H,35,36)/b28-23-
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 DQP 1105

DescriptionNoncompetitive NMDA receptor antagonist; displays over 50-fold selectivity for GluN2D- and GluN2C-containing receptors over GluN2B-, GluK2-, GluA1- and GluN2A-containing receptors (IC50 values are 2.7, 8.5, 121, 153, 198 and 206 μM, respectively). Reduces frequency of channel opening.

DQP 1105 Dilution Calculator

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DQP 1105 Molarity Calculator

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Preparing Stock Solutions of DQP 1105

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.7908 mL 8.9538 mL 17.9077 mL 35.8153 mL 44.7692 mL
5 mM 0.3582 mL 1.7908 mL 3.5815 mL 7.1631 mL 8.9538 mL
10 mM 0.1791 mL 0.8954 mL 1.7908 mL 3.5815 mL 4.4769 mL
50 mM 0.0358 mL 0.1791 mL 0.3582 mL 0.7163 mL 0.8954 mL
100 mM 0.0179 mL 0.0895 mL 0.1791 mL 0.3582 mL 0.4477 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 DQP 1105

Glutamatergic synaptic currents of nigral dopaminergic neurons follow a postnatal developmental sequence.[Pubmed:26074777]

Front Cell Neurosci. 2015 May 29;9:210.

The spontaneous activity pattern of adult dopaminergic (DA) neurons of the substantia nigra pars compacta (SNc) results from interactions between intrinsic membrane conductances and afferent inputs. In adult SNc DA neurons, low-frequency tonic background activity is generated by intrinsic pacemaker mechanisms, whereas burst generation depends on intact synaptic inputs in particular the glutamatergic ones. Tonic DA release in the striatum during pacemaking is required to maintain motor activity, and burst firing evokes phasic DA release, necessary for cue-dependent learning tasks. However, it is still unknown how the firing properties of SNc DA neurons mature during postnatal development before reaching the adult state. We studied the postnatal developmental profile of spontaneous and evoked AMPA and NMDA (N-Methyl-D-aspartic acid) receptor-mediated excitatory postsynaptic currents (EPSCs) in SNc DA neurons in brain slices from immature (postnatal days P4-P10) and young adult (P30-P50) tyrosine hydroxylase (TH)-green fluorescent protein mice. We found that somato-dendritic fields of SNc DA neurons are already mature at P4-P10. In contrast, spontaneous glutamatergic EPSCs show a developmental sequence. Spontaneous NMDA EPSCs in particular are larger and more frequent in immature SNc DA neurons than in young adult ones and have a bursty pattern. They are mediated by GluN2B and GluN2D subunit-containing NMDA receptors. The latter generate long-lasting, DQP 1105-sensitive, spontaneous EPSCs, which are transiently recorded during this early period. Due to high NMDA activity, immature SNc DA neurons generate large and long lasting NMDA receptor-dependent (APV-sensitive) bursts in response to the stimulation of the subthalamic nucleus. We conclude that the transient high NMDA activity allows calcium influx into the dendrites of developing SNc DA neurons.

Mechanism for noncompetitive inhibition by novel GluN2C/D N-methyl-D-aspartate receptor subunit-selective modulators.[Pubmed:21807990]

Mol Pharmacol. 2011 Nov;80(5):782-95.

The compound 4-(5-(4-bromophenyl)-3-(6-methyl-2-oxo-4-phenyl-1,2-dihydroquinolin-3-yl)-4,5-dih ydro-1H-pyrazol-1-yl)-4-oxobutanoic acid (DQP-1105) is a representative member of a new class of N-methyl-d-aspartate (NMDA) receptor antagonists. DQP-1105 inhibited GluN2C- and GluN2D-containing receptors with IC(50) values that were at least 50-fold lower than those for recombinant GluN2A-, GluN2B-, GluA1-, or GluK2-containing receptors. Inhibition was voltage-independent and could not be surmounted by increasing concentrations of either coagonist, glutamate or glycine, consistent with a noncompetitive mechanism of action. DQP-1105 inhibited single-channel currents in excised outside-out patches without significantly changing mean open time or single-channel conductance, suggesting that DQP inhibits a pregating step without changing the stability of the open pore conformation and thus channel closing rate. Evaluation of DQP-1105 inhibition of chimeric NMDA receptors identified two key residues in the lower lobe of the GluN2 agonist binding domain that control the selectivity of DQP-1105. These data suggest a mechanism for this new class of inhibitors and demonstrate that ligands can access, in a subunit-selective manner, a new site located in the lower, membrane-proximal portion of the agonist-binding domain.

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