| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
UBP301 acts as a competitive antagonist at both AMPA (GluA2 subunit, Ki = 8.2 μM) and kainate (GluK1 subunit, Ki = 2.3 μM) receptors, with moderate selectivity for kainate receptors over AMPA receptors (∼3.5-fold) [1]
|
|---|---|
| ln Vitro |
In Vitro: [1]
<｜place▁holder▁no▁797｜> In recombinant HEK293 cells expressing GluK1 receptors, UBP301 (10 μM) inhibited kainate-evoked currents by 92 ± 3% (IC50 = 0.9 μM), showing potent antagonism. Schild plot analysis yielded a slope of 1.02 ± 0.05, confirming competitive antagonism at the glutamate binding site. For AMPA receptors (GluA2-expressing cells), UBP301 (100 μM) reduced AMPA-induced currents by 85 ± 4% (IC50 = 32 μM), demonstrating weaker activity compared to kainate receptors. The pA2 value was 4.7 ± 0.2, indicating lower affinity [1] |
| Enzyme Assay |
Enzyme Assay: [1]
Radioligand displacement assays were conducted using [3H]kainate on rat cortical membranes. Membranes were incubated with UBP301 (1 nM–300 μM) and 15 nM [3H]kainate in 50 mM Tris-HCl buffer (pH 7.4, 4°C) for 45 min. Bound ligand was separated via vacuum filtration through GF/B filters, washed with ice-cold buffer, and quantified by liquid scintillation spectrometry to calculate Ki values [1] |
| References | |
| Additional Infomation |
Additional Info: [1]
UBP301 is a 5-iodowillardiine analog designed to optimize steric bulk at the N3-position for enhanced receptor subtype discrimination. Its iodine substitution increases hydrophobic interactions within the ligand-binding domain, improving kainate receptor affinity over earlier derivatives. Serves as a key pharmacological tool for dissecting AMPA/kainate receptor contributions to excitatory neurotransmission, particularly in studies of synaptic plasticity and excitotoxicity [1] |
| Molecular Formula |
C15H14IN3O6
|
|---|---|
| Molecular Weight |
516.65614
|
| Exact Mass |
458.993
|
| CAS # |
569371-10-4
|
| Related CAS # |
UBP301 hydrochloride
|
| PubChem CID |
6604913
|
| Appearance |
Typically exists as solid at room temperature
|
| LogP |
0.473
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
25
|
| Complexity |
614
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
C1=C(C=CC(=C1)C(=O)O)CN2C(=O)C(=CN(C[C@@H](C(=O)O)N)C2=O)I
|
| InChi Key |
JHSYCOCOIYSZGI-NSHDSACASA-N
|
| InChi Code |
InChI=1S/C15H14IN3O6/c16-10-6-18(7-11(17)14(23)24)15(25)19(12(10)20)5-8-1-3-9(4-2-8)13(21)22/h1-4,6,11H,5,7,17H2,(H,21,22)(H,23,24)/t11-/m0/s1
|
| Chemical Name |
4-[[3-[(2S)-2-amino-2-carboxyethyl]-5-iodo-2,6-dioxopyrimidin-1-yl]methyl]benzoic acid
|
| Synonyms |
UBP-301; 569371-10-4; UBP 301; UBP301; (AS)-alpha-AMINO-3-[(4-CARBOXYPHENYL)METHYL]-3,4-DIHYDRO-5-IODO-2,4-DIOXO-1(2H)-PYRIMIDINEPROPANOIC ACID; 4-[[3-[(2S)-2-amino-2-carboxyethyl]-5-iodo-2,6-dioxopyrimidin-1-yl]methyl]benzoic acid; CHEMBL200309; NCGC00025285-01;
|
| 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 |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO: 100 mg/mL (217.77 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (10.89 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 50.0 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: ≥ 5 mg/mL (10.89 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 50.0 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: ≥ 5 mg/mL (10.89 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 | 1.9355 mL | 9.6775 mL | 19.3551 mL | |
| 5 mM | 0.3871 mL | 1.9355 mL | 3.8710 mL | |
| 10 mM | 0.1936 mL | 0.9678 mL | 1.9355 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
