| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg | |||
| 500mg | |||
| Other Sizes |
| Targets |
Excitatory amino acid transporter subtype 1 (EAAT1), with IC50 = 0.66 μM. EAAT1 (also known as GLAST) is a glial glutamate transporter responsible for the clearance of glutamate from the synaptic cleft. Inhibition of EAAT1 increases extracellular glutamate levels, which can be used to study the role of glutamate transport in synaptic transmission, plasticity, and excitotoxicity.
|
|---|---|
| ln Vitro |
Peptide YY (pig) (10 μg/mL) and human Irish pancreas (PP) are also in vogue, that is, unique to PYY antisera, and both could have a beneficial, cosmetic effect in controlling any pancreatic islet fishery [2].
UCPH-101 potently inhibits EAAT1-mediated glutamate uptake with an IC50 of 0.66 μM in EAAT1-HEK293 cells. The compound is a selective EAAT1 inhibitor. Its inhibition of glutamate uptake increases extracellular glutamate concentrations, which can enhance glutamatergic neurotransmission or induce excitotoxicity depending on the context. This makes UCPH-101 a valuable tool for studying the physiological and pathological roles of EAAT1 in the central nervous system. |
| ln Vivo |
In vivo effects of UCPH-101 have been studied in rodent models. As an EAAT1 inhibitor, the compound increases extracellular glutamate levels in the brain, which can affect synaptic transmission, plasticity, and behavior. UCPH-101 is used to study the role of glutamate transporters in neurological and psychiatric disorders. The compound is a selective EAAT1 inhibitor that is widely used in neuroscience research. Detailed in vivo efficacy data in specific disease models are limited in publicly available sources.
|
| Enzyme Assay |
EAAT1 inhibition assays are performed using HEK-293 cells stably or transiently expressing human EAAT1. Cells are seeded in 96-well plates and allowed to adhere. Uptake assays are initiated by adding [3H]-D-aspartate ([3H]-D-Asp) or [3H]-glutamate in uptake buffer (140 mM NaCl, 2.5 mM KCl, 1.2 mM CaCl2, 1.2 mM MgCl2, 10 mM HEPES pH 7.4) with varying concentrations of UCPH-101. The reaction is incubated at 37°C for 5-10 minutes and terminated by washing with ice-cold buffer. Cells are lysed and radioactivity is quantified by scintillation counting. Non-specific uptake is determined using sodium-free buffer or in the presence of excess unlabeled substrate. IC50 values are determined by non-linear regression analysis. Each concentration is tested in triplicate.
|
| Cell Assay |
Cellular EAAT1 inhibition is evaluated in HEK-293 cells expressing EAAT1 or in primary astrocyte cultures. Cells are cultured in appropriate media at 37°C with 5% CO2 and treated with UCPH-101 at various concentrations (0.01-100 μM) for 15-60 minutes. Glutamate uptake is measured using [3H]-glutamate or [3H]-D-aspartate as described above. Extracellular glutamate levels can be measured using glutamate biosensors or HPLC. Cell viability is assessed using MTT or LDH assays to ensure compound concentrations are not cytotoxic. Each experiment includes known EAAT inhibitors (e.g., DL-TBOA) as positive controls and vehicle controls.
|
| Animal Protocol |
In vivo studies are conducted in rodents (rats or mice). UCPH-101 is administered via intracerebroventricular (ICV) injection or systemic administration (intraperitoneal or intravenous) depending on blood-brain barrier permeability. Microdialysis is used to measure extracellular glutamate levels in specific brain regions. Behavioral studies may be conducted to evaluate the effects of EAAT1 inhibition on learning, memory, anxiety, or pain sensitivity. Brain tissue is collected for histology and biochemical analysis. Sample sizes typically range from 6-10 animals per group. Detailed protocols are not publicly available.
|
| ADME/Pharmacokinetics |
Limited PK data are available. UCPH-101 has a molecular weight of 422.48 g/mol. Solubility: soluble in DMSO. Purity: typically ≥98%. Storage: typically at -20°C. Bioavailability, brain penetration, half-life, and tissue distribution data are not publicly available. The compound is primarily used as a research tool for in vitro and in vivo studies of EAAT1 function.
|
| Toxicity/Toxicokinetics |
Limited toxicology data are available for UCPH-101. As an EAAT1 inhibitor that increases extracellular glutamate levels, potential toxicities may include excitotoxicity at high doses. Standard toxicology studies would include acute toxicity in rodents, genotoxicity screening, and evaluation of effects on the central nervous system. No clinical trials have been reported for this compound. The compound is intended for research use only.
|
| References | |
| Additional Infomation |
UCPH-101 is also known as 2-amino-5,6,7,8-tetrahydro-4-(4-methoxyphenyl)-7-(naphthalen-1-yl)-5-oxo-4H-chromene-3-carbonitrile. It is a potent and selective EAAT1 inhibitor with an IC50 of 0.66 μM. It is widely used in neuroscience research to study the role of glutamate transporters in synaptic transmission and plasticity. No clinical trials or regulatory approvals have been reported. The compound is for research use only.
|
| Molecular Formula |
C27H22N2O3
|
|---|---|
| Molecular Weight |
422.475186824799
|
| Exact Mass |
422.163
|
| CAS # |
1118460-77-7
|
| Related CAS # |
1118460-77-7;
|
| PubChem CID |
25223366
|
| Appearance |
White to off-white solid powder
|
| LogP |
5.757
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
32
|
| Complexity |
857
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
YBMGNDPBARCLFT-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C27H22N2O3/c1-31-19-11-9-17(10-12-19)25-22(15-28)27(29)32-24-14-18(13-23(30)26(24)25)21-8-4-6-16-5-2-3-7-20(16)21/h2-12,18,25H,13-14,29H2,1H3
|
| Chemical Name |
2-amino-4-(4-methoxyphenyl)-7-naphthalen-1-yl-5-oxo-4,6,7,8-tetrahydrochromene-3-carbonitrile
|
| 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 : ≥ 50 mg/mL (~118.35 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.92 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 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 25.0 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3670 mL | 11.8349 mL | 23.6698 mL | |
| 5 mM | 0.4734 mL | 2.3670 mL | 4.7340 mL | |
| 10 mM | 0.2367 mL | 1.1835 mL | 2.3670 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
