| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg | |||
| Other Sizes |
| Targets |
GluK1 (formerly GLUK5) kainate receptor. UBP-310 is a selective antagonist at the GluK1 kainate receptor with an IC50 of 130 nM. It displays 12,700-fold selectivity for GluK1 over GluK2 and 830-fold selectivity over GluK2. It also blocks recombinant homomeric GluK3 receptors and has no activity at mGlu group I or NMDA receptors at concentrations up to 10 μM.
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| ln Vitro |
UBP310 is 12,700 times more selective for GluR5 than GluR6 and 830 times more selective for GluR5 than GluR2 and binds to GluR5 S1S2 with an affinity of 130 nM [1].
In vitro, UBP-310 binds to the GluK1 S1S2 ligand-binding domain with an affinity (Kd) of 130 nM. It exhibits 12,700-fold selectivity for GluK1 versus GluK6 and 830-fold selectivity versus GluK2. The compound has been shown to block sustained kainate receptor activation that leads to AMPA receptor endocytosis and induces long-term depression (LTD) in hippocampal neurons. UBP-310 also blocks recombinant homomeric GluK7 receptors. |
| ln Vivo |
In vivo, UBP-310 has been used in acute hippocampal slice preparations where kainate application caused a significant loss of GluA2-containing AMPARs from synapses and long-lasting depression of AMPAR excitatory postsynaptic currents in CA1. The compound blocks KAR-evoked loss of surface AMPARs, indicating that KAR-LTDAMPAR requires KAR channel activity. It has also been used in studies of hypoxia-induced seizures in neonatal mice.
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| Enzyme Assay |
Non-cell receptor binding assays are performed using membrane preparations from cells expressing recombinant GluK1 or other kainate receptor subunits. Radioligand binding studies are conducted using [³H]kainate or [³H]domoate as tracers. Membranes are incubated with the radioligand and varying concentrations of UBP-310 (0.001-100 μM). Nonspecific binding is determined with excess unlabeled kainate. After incubation at 4°C for 60-120 minutes, bound and free ligand are separated by filtration through glass fiber filters, and radioactivity is measured by scintillation counting. IC₅₀ and Ki values are calculated from competition curves.
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| Cell Assay |
Cellular assays are performed using HEK-293 or CHO cells transfected with GluK1 or other kainate receptor subunits. Whole-cell patch-clamp electrophysiology is used to record kainate-evoked currents in the presence of UBP-310 at concentrations ranging from 0.01-100 μM. Alternatively, calcium imaging using fluorescent indicators (e.g., Fura-2) can be used to measure receptor-mediated calcium influx. The IC₅₀ for inhibition of kainate-evoked responses is determined from dose-response curves. For hippocampal neurons, UBP-310 is applied during kainate treatment to assess its effect on AMPA receptor surface expression and LTD.
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| Animal Protocol |
In vivo animal studies are conducted in rodent models. UBP-310 is typically administered via intracerebroventricular (i.c.v.) injection or locally applied to brain slices for electrophysiological recordings. In hypoxia-induced seizure models, the compound is used to investigate the role of kainate receptors in seizure pathophysiology. Doses and routes of administration vary depending on the experimental paradigm. For slice electrophysiology, UBP-310 is applied in the perfusing artificial cerebrospinal fluid at concentrations of 1-10 μM. Behavioral and electrophysiological endpoints are assessed.
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| ADME/Pharmacokinetics |
Published pharmacokinetic data for UBP-310 are limited. As a small molecule (molecular weight: 353.35), it is expected to have reasonable brain penetration due to its ability to act on central kainate receptors. The compound is typically used in ex vivo slice preparations or via direct central administration in vivo. Further studies on oral bioavailability, half-life, and metabolism are not well characterized.
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| Toxicity/Toxicokinetics |
Comprehensive toxicology data for UBP-310 are not available in the public domain. In published studies, the compound was well-tolerated at concentrations used for electrophysiological recordings in brain slices. No significant toxicity has been reported at effective concentrations. Standard safety pharmacology studies would be required for therapeutic development. The compound is for research use only and not for human therapeutic applications.
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| References | |
| Additional Infomation |
GluR5 antagonist; structure can be found in the first article.
UBP-310 is a research compound developed for studying kainate receptor function in neuroscience. It is a highly selective GluK1 antagonist that has been used to demonstrate the role of kainate receptors in hippocampal long-term depression (KAR-LTDAMPAR). The compound is also known as (S)-1-(2-Amino-2-carboxyethyl)-3-(2-carboxy-thiophene-3-yl-methyl)-5-methylpyrimidine-2,4-dione. UBP-310 is not approved for clinical use and is intended for laboratory research purposes only. |
| Molecular Formula |
C14H15N3O6S
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|---|---|
| Molecular Weight |
353.350402116776
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| Exact Mass |
353.068
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| CAS # |
902464-46-4
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| PubChem CID |
6420160
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| Appearance |
White to off-white solid powder
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| LogP |
0.238
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
24
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| Complexity |
607
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CC1=CN(C(=O)N(C1=O)CC2=C(SC=C2)C(=O)O)C[C@@H](C(=O)O)N
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| InChi Key |
ZTAZUCRXCRXNSU-VIFPVBQESA-N
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| InChi Code |
InChI=1S/C14H15N3O6S/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,5-6,15H2,1H3,(H,19,20)(H,21,22)/t9-/m0/s1
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| Chemical Name |
3-[[3-[(2S)-2-amino-2-carboxyethyl]-5-methyl-2,6-dioxopyrimidin-1-yl]methyl]thiophene-2-carboxylic acid
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
1M HCl : 30 mg/mL (~84.90 mM)
DMSO : ~3.57 mg/mL (~10.10 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.36 mg/mL (1.02 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 3.6 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 0.36 mg/mL (1.02 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 3.6 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. View More
Solubility in Formulation 3: ≥ 0.36 mg/mL (1.02 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8301 mL | 14.1503 mL | 28.3006 mL | |
| 5 mM | 0.5660 mL | 2.8301 mL | 5.6601 mL | |
| 10 mM | 0.2830 mL | 1.4150 mL | 2.8301 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.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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