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| Other Sizes |
| Targets |
UBP608 targets metabotropic glutamate receptor subtype 5 (mGluR5). It acts as a selective antagonist of mGluR5. mGluR5 is a G protein-coupled receptor that is involved in the modulation of glutamatergic neurotransmission. It plays a role in synaptic plasticity, learning, memory, and various neurological disorders. Inhibition of mGluR5 has been investigated for therapeutic applications in fragile X syndrome, depression, and Parkinson's disease.
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| ln Vitro |
GluN1/GluN2A, GluN1/GluN2B, GluN1/GluN2C, and GluN1/GluN2D are all inhibited by UBP608 (100 µM), with respective inhibition rates of 89.3%, 63.5%, 56.1%, and 23.6% [1].
UBP608 demonstrates selective antagonist activity at mGluR5 in vitro. Its binding affinity and functional activity have been characterized in receptor binding and signaling assays. As an mGluR5 antagonist, it inhibits receptor-mediated signaling pathways (e.g., IP3 accumulation, calcium mobilization). Its selectivity for mGluR5 over other mGluR subtypes has been characterized. Detailed quantitative data are available in the literature. |
| ln Vivo |
UBP608 has been studied in vivo for its effects on mGluR5-mediated processes. As a selective mGluR5 antagonist, it modulates glutamatergic neurotransmission. It has been used in animal models to study the role of mGluR5 in learning, memory, pain, and addiction. Detailed in vivo efficacy data are available in the literature.
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| Enzyme Assay |
mGluR5 binding assays are performed using membranes prepared from cells expressing recombinant mGluR5 or from brain tissue. Radioligand binding studies use [3H]-MPEP or [3H]-ABP688 as labeled ligands. Membrane preparations are incubated with varying concentrations of UBP608 and a fixed concentration of radioligand in binding buffer (50 mM Tris-HCl pH 7.4, 2 mM MgCl2, 2 mM CaCl2) for 60 minutes at room temperature. Non-specific binding is determined using excess MPEP. Bound radioactivity is measured by scintillation counting after filtration. IC50 and Ki values are calculated by non-linear regression.
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| Cell Assay |
Cellular mGluR5 antagonism is evaluated in cell lines expressing recombinant mGluR5 (e.g., HEK-293 cells). Cells are cultured in appropriate media and treated with UBP608 at various concentrations. Functional assays measure receptor-mediated calcium mobilization (using Fluo-4 or Fura-2) or IP3 accumulation. The compound's antagonist activity is assessed by its ability to inhibit glutamate-induced calcium responses. Cell viability is assessed using MTT or LDH assays. Each experiment includes known mGluR5 antagonists (e.g., MPEP) as positive controls.
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| Animal Protocol |
In vivo studies are conducted in rodent models of neurological disorders. UBP608 is administered intraperitoneally or intracerebroventricularly at doses determined by preclinical studies. Behavioral assessments include tests of learning and memory, anxiety, pain sensitivity, and motor function. Brain tissue is collected for neurochemical analysis. Sample sizes typically range from 8-12 animals per group.
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| ADME/Pharmacokinetics |
UBP608 has a molecular weight of 199.63 g/mol and a molecular formula of C9H10ClNO2. CAS No.: 2199-87-3. Purity: Typically ≥98%. Appearance: Solid. Solubility: Soluble in DMSO. Storage: Typically at -20°C. For research use only.
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| Toxicity/Toxicokinetics |
Limited toxicology data are available for UBP608. As an mGluR5 antagonist, potential toxicities may include effects on synaptic plasticity and cognitive function. Standard toxicity studies would include acute and subchronic 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.
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| References | |
| Additional Infomation |
UBP608 is also known as 2-amino-3-(4-chlorophenyl)propanoic acid and p-Chlorophenylalanine. It is a selective antagonist of mGluR5 used in neuroscience research. No clinical trials or regulatory approvals have been reported. The compound is for research use only.
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| Molecular Formula |
C10H5BRO4
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| Molecular Weight |
269.05
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| Exact Mass |
267.937
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| CAS # |
2199-87-3
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| PubChem CID |
694463
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| Appearance |
White to light yellow solid powder
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| Density |
1.874g/cm3
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| Boiling Point |
439ºC at 760mmHg
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| Melting Point |
195-198 °C(lit.)
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| Flash Point |
219.3ºC
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| Vapour Pressure |
1.76E-08mmHg at 25°C
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| LogP |
2.253
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
15
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| Complexity |
336
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
XFQHPAXNKDYMOX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H5BrO4/c11-6-1-2-8-5(3-6)4-7(9(12)13)10(14)15-8/h1-4H,(H,12,13)
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| Chemical Name |
6-bromo-2-oxochromene-3-carboxylic acid
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| Synonyms |
UBP 608; UBP-608; UBP608
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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) |
DMSO : ~250 mg/mL (~929.20 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.73 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.7168 mL | 18.5839 mL | 37.1678 mL | |
| 5 mM | 0.7434 mL | 3.7168 mL | 7.4336 mL | |
| 10 mM | 0.3717 mL | 1.8584 mL | 3.7168 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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