UCPH-101 |
Catalog No.GC19365
One-Click Copy Product Info
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UCPH-101 is an inhibitor of Excitatory Amino Acid Transporter 1 (EAAT1), with an IC50 value of 0.66μM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1118460-77-7
Sample solution is provided at 25 µL, 10mM.
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UCPH-101 is an inhibitor of Excitatory Amino Acid Transporter 1 (EAAT1), with an IC50 value of 0.66μM[1]. UCPH-101 acts as a slow-binding, non-competitive EAAT1 inhibitor; it blocks the translocation step within the transport cycle rather than other partial reactions[2]. UCPH-101 is capable of blocking the neuroprotective effects of dexmedetomidine and guanfacine[3]. UCPH-101 induces glioblastoma cell death by promoting the intracellular accumulation of glutamate and has been shown to significantly improve survival in mouse models of glioma[4].
In vitro, treatment of murine MA9-1 cells and human U937 cells with UCPH-101 (20μM) for 6-24 hours significantly increased apoptotic levels in both cell lines, resulting in a decrease in cells in the G1 phase and a corresponding increase in cells in the S and G2/M phases[5]. Treatment of GL261-NS cells, GBM-NS cells, and astrocytes with UCPH-101 (10μM) significantly elevated apoptotic levels in the GL261-NS and GBM-NS cells, while having no effect on the apoptotic levels of the astrocytes[6].
In vivo, intracranial administration of UCPH-101 (10nmol/μL) to mice bearing glioma xenografts significantly improved survival rates. Furthermore, the treatment significantly disrupted the tissue architecture of the brain gliomas, significantly downregulated the expression levels of the glutamate-aspartate transporter (GLAST) within the tumor tissue, and significantly upregulated the expression levels of cleaved Caspase-3[6].
References:
[1] Huynh T H V, Abrahamsen B, Madsen K K, et al. Design, synthesis and pharmacological characterization of coumarin-based fluorescent analogs of excitatory amino acid transporter subtype 1 selective inhibitors, UCPH-101 and UCPH-102[J]. Bioorganic & medicinal chemistry, 2012, 20(23): 6831-6839.
[2] Dong Y. Functional Studies of Amino Acid Transporters from the Solute Carrier SLC1 and SLC38 Families[D]. State University of New York at Binghamton, 2024.
[3] Mei B, Xu X, Weng J, et al. Activating astrocytic α2A adrenoceptors in hippocampus reduces glutamate toxicity to attenuate sepsis-associated encephalopathy in mice[J]. Brain, Behavior, and Immunity, 2024, 117: 376-398.
[4] Corbetta C, Di Ianni N, Bruzzone M G, et al. Altered function of the glutamate aspartate transporter GLAST in glioblastoma[J]. bioRxiv, 2018: 287623.
[5] Tirado H A, Balasundaram N, Jacobs J, et al. The EAAT1 aspartate/glutamate transporter is dispensable for acute myeloid leukemia cell growth and response to therapy[J]. Plos one, 2026, 21(2): e0329048.
[6] Corbetta C, Di Ianni N, Bruzzone M G, et al. Altered function of the glutamate–aspartate transporter GLAST, a potential therapeutic target in glioblastoma[J]. International journal of cancer, 2019, 144(10): 2539-2554.
| Cell experiment [1]: | |
Cell lines | Mouse MA9-1 and human U937 cell line |
Preparation Method | Mouse MA9-1 cells and human U937 cells were cultured separately and subsequently treated with UCPH-101 at a final concentration of 20µM. After 24h of treatment, the cells were harvested, and apoptosis was detected via flow cytometry using Annexin V-FITC/PI double staining; a treatment group with 250µM TFB-TBOA was included as a control. An additional group of cells was treated with 20µM UCPH-101 for 6h, followed by fixation and PI staining, to analyze cell cycle distribution via flow cytometry. |
Reaction Conditions | 20µM; 6, 24h |
Applications | Following treatment with 20µM UCPH-101 for 24h, apoptosis increased in both murine MA9-1 cells and human U937 cells; conversely, treatment with 250µM TFB-TBOA did not affect cell viability. Cell cycle analysis revealed that UCPH-101 resulted in a decrease in cells in the G1 phase, accompanied by a corresponding increase in cells in the S and G2/M phases. |
| Animal experiment [2]: | |
Animal models | Female C57BL/6 N mice、CD1 nude mice |
Preparation Method | Five weeks-old female C57BL/6 N (n=10/group for survival studies) and CD1 nude (nude CD1 (HO): CD1-Foxn1nu) mice (n=7/group for survival studies) were intracranially injected with 1×105 GL261-NS or GSCs respectively, in 2μL PBS 1×. The coordinates, with respect to the bregma, were 0.7mm post, 3mm left lateral, 3.5mm deep, and within the nucleus caudatum. Five weeks-old female CD1 nude mice (n=7/group for survival, n=3/group for histolog ical studies); were intracranially injected with 1×105 scram bled or shGLAST GSCs. Five weeks-old female C57BL/6 N mice (n = 7/group for survival analysis; n=4 for histological studies) were injected with 1×105 GL261-NS and treated with 10nmol/μL of UCPH-101 or DMSO as the negative control, 9 days after tumor implantation. For survival studies mice were monitored every day and when suf fering euthanized; for histological studies mice brains were collected and fixed in 4% paraformaldehyde. |
Dosage form | 10nmol/μL; intracranially injected |
Applications | In glioma-bearing mice, a single intratumoral injection of UCPH-101 significantly increased survival by decreasing GLAST expression and inducing apoptosis. |
References: | |
| Cas No. | 1118460-77-7 | SDF | |
| Canonical SMILES | O=C(C1)C2=C(OC(N)=C(C#N)C2C3=CC=C(OC)C=C3)CC1C4=CC=CC5=C4C=CC=C5 | ||
| Formula | C27H22N2O3 | M.Wt | 422.48 |
| Solubility | DMSO : ≥ 110 mg/mL (260.37 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.367 mL | 11.8349 mL | 23.6698 mL |
| 5 mM | 473.4 μL | 2.367 mL | 4.734 mL |
| 10 mM | 236.7 μL | 1.1835 mL | 2.367 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 8 reference(s) in Google Scholar.)