UBP 310CAS# 902464-46-4 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
Cas No. | 902464-46-4 | SDF | Download SDF |
PubChem ID | 76543637 | Appearance | Powder |
Formula | C14H15N3O6S | M.Wt | 353.35 |
Type of Compound | N/A | Storage | Desiccate at -20°C |
Solubility | Soluble to 100 mM in DMSO | ||
Chemical Name | 3-[[3-(2-amino-2-carboxyethyl)-5-methylidene-2,6-dioxopyrimidin-3-ium-1-yl]methyl]thiophene-2-carboxylic acid | ||
SMILES | C=C1C=[N+](C(=O)N(C1=O)CC2=C(SC=C2)C(=O)O)CC(C(=O)O)N | ||
Standard InChIKey | JKFBXNLABOXGTM-UHFFFAOYSA-O | ||
Standard InChI | InChI=1S/C14H13N3O6S/c1-7-4-16(6-9(15)12(19)20)14(23)17(11(7)18)5-8-2-3-24-10(8)13(21)22/h2-4,9H,1,5-6,15H2,(H-,19,20,21,22)/p+1 | ||
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. |
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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. |
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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. |
Description | GLUK5 kainate receptor antagonist (IC50 = 130 nM); also blocks recombinant homomeric GLUK7 receptors. Displays 12,700-fold selectivity for GLUK5 over GLUK6. Exhibits no activity at mGlu group I or NMDA receptors at concentrations of up to 10 μM. Apparent KD value is 18 ± 4 nM for depression of kainate responses on the dorsal root. |
UBP 310 Dilution Calculator
UBP 310 Molarity Calculator
1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
1 mM | 2.8301 mL | 14.1503 mL | 28.3006 mL | 56.6011 mL | 70.7514 mL |
5 mM | 0.566 mL | 2.8301 mL | 5.6601 mL | 11.3202 mL | 14.1503 mL |
10 mM | 0.283 mL | 1.415 mL | 2.8301 mL | 5.6601 mL | 7.0751 mL |
50 mM | 0.0566 mL | 0.283 mL | 0.566 mL | 1.132 mL | 1.415 mL |
100 mM | 0.0283 mL | 0.1415 mL | 0.283 mL | 0.566 mL | 0.7075 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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Antagonism of recombinant and native GluK3-containing kainate receptors.[Pubmed:18761361]
Neuropharmacology. 2009 Jan;56(1):131-40.
A number of kainate receptor antagonists have shown selectivity for receptors containing the GluK1 subunit. Here, we analyze the effects of these GluK1 antagonists on currents mediated by recombinant homomeric GluK3 and heteromeric GluK2/3 receptors expressed in HEK 293 cells and activated by fast application of glutamate. We show that, amongst these compounds, UBP302, UBP310 and UBP316 effectively block recombinant homomeric GluK3 receptors. However, these antagonists are ineffective in blocking homomeric GluK2 or heteromeric GluK2/3 receptors. In addition, these antagonists do not affect presynaptic kainate receptors at mouse hippocampal mossy fibre synapses, which are thought to be composed of GluK2 and GluK3 subunits. Moreover, the AMPA receptor-selective non-competitive antagonist GYKI 53655 blocks, at high concentrations, GluK3-containing receptors and decreases short-term plasticity at mossy fibre synapses. These results expand the range of targets of kainate receptor antagonists and provide pharmacological tools to study the elusive mechanisms of neurotransmitter control by presynaptic kainate receptors.
Synthesis and pharmacological characterization of N3-substituted willardiine derivatives: role of the substituent at the 5-position of the uracil ring in the development of highly potent and selective GLUK5 kainate receptor antagonists.[Pubmed:17348638]
J Med Chem. 2007 Apr 5;50(7):1558-70.
Some N3-substituted analogues of willardiine such as 11 and 13 are selective kainate receptor antagonists. In an attempt to improve the potency and selectivity for kainate receptors, a range of analogues of 11 and 13 were synthesized with 5-substituents on the uracil ring. An X-ray crystal structure of the 5-methyl analogue of 13 bound to GLUK5 revealed that there was allowed volume around the 4- and 5-positions of the thiophene ring, and therefore the 4,5-dibromo and 5-phenyl (67) analogues were synthesized. Compound 67 (ACET) demonstrated low nanomolar antagonist potency on native and recombinant GLUK5-containing kainate receptors (KB values of 7 +/- 1 and 5 +/- 1 nM for antagonism of recombinant human GLUK5 and GLUK5/GLUK2, respectively) but displayed IC50 values >100 microM for antagonism of GLUA2, GLUK6, or GLUK6/GLUK2.
Crystal structures of the kainate receptor GluR5 ligand binding core dimer with novel GluR5-selective antagonists.[Pubmed:16540562]
J Neurosci. 2006 Mar 15;26(11):2852-61.
Glutamate receptor (GluR) ion channels mediate fast synaptic transmission in the mammalian CNS. Numerous crystallographic studies, the majority on the GluR2-subtype AMPA receptor, have revealed the structural basis for binding of subtype-specific agonists. In contrast, because there are far fewer antagonist-bound structures, the mechanisms for antagonist binding are much less well understood, particularly for kainate receptors that exist as multiple subtypes with a distinct biology encoded by the GluR5-7, KA1, and KA2 genes. We describe here high-resolution crystal structures for the GluR5 ligand-binding core complex with UBP302 and UBP310, novel GluR5-selective antagonists. The crystal structures reveal the structural basis for the high selectivity for GluR5 observed in radiolabel displacement assays for the isolated ligand binding cores of the GluR2, GluR5, and GluR6 subunits and during inhibition of glutamate-activated currents in studies on full-length ion channels. The antagonists bind via a novel mechanism and do not form direct contacts with the E723 side chain as occurs in all previously solved AMPA and kainate receptor agonist and antagonist complexes. This results from a hyperextension of the ligand binding core compared with previously solved structures. As a result, in dimer assemblies, there is a 22 A extension of the ion channel linkers in the transition from antagonist- to glutamate-bound forms. This large conformational change is substantially different from that described for AMPA receptors, was not possible to predict from previous work, and suggests that glutamate receptors are capable of much larger movements than previously thought.