| Identification | Back Directory | [Name]
UCPH-102 | [CAS]
1229591-56-3 | [Synonyms]
UCPH-102
UCPH-102 >=98% (HPLC)
UCPH-102, EAAT1 inhibitor
4H-1-Benzopyran-3-carbonitrile, 2-amino-5,6,7,8-tetrahydro-4-methyl-7-(1-naphthalenyl)-5-oxo- | [Molecular Formula]
C21H18N2O2 | [MDL Number]
MFCD30537549 | [MOL File]
1229591-56-3.mol | [Molecular Weight]
330.38 |
| Chemical Properties | Back Directory | [Boiling point ]
610.7±55.0 °C(Predicted) | [density ]
1.30±0.1 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: 20mg/mL, clear | [form ]
powder | [pka]
3.39±0.60(Predicted) | [color ]
white to beige | [InChIKey]
XZQMHUGTNOOYFX-UHFFFAOYSA-N | [SMILES]
O=C(C1)C2=C(OC(N)=C(C#N)C2C)CC1C3=C(C=CC=C4)C4=CC=C3 |
| Hazard Information | Back Directory | [Uses]
UCPH-102 is a highly selective EAAT1 inhibitor with an IC50 of 0.43 μM. UCPH-102 exhibits a specific anti-proliferative effect on T-ALL cells. UCPH-102 also shows good blood-brain permeability, which can be used in studies of amyotrophic lateral sclerosis, Alzheimer’s disease, chronic pain and obsessive compulsive disorder[1][2][3][4]. | [Biological Activity]
UCPH-102 is a selective inhibitor of the Excitatory Amino Acid Transporter subtype-1 (EAAT1GLAST) with an IC50 value of 420 nM for EAAT1 and >300 μM for EAAT2-5. UCPH-102 has been shown to cross the blood-brain barrierso should become a valuable tool for studying the role of EAAT1 in brain. | [IC 50]
EAAT1 | [References]
[1] Huynh TH, 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. Bioorg Med Chem. 2012 Dec 1;20(23):6831-9. DOI:10.1016/j.bmc.2012.09.049
[2] Haym I, et al. Bioavailability Studies and in vitro Profiling of the Selective Excitatory Amino Acid Transporter Subtype 1 (EAAT1) Inhibitor UCPH-102. ChemMedChem. 2016 Feb 17;11(4):403-19. DOI:10.1002/cmdc.201500527
[3] Stanulovi? V S, et al. Proliferation and Survival of T-cell Acute Lymphoblastic Leukaemia Depends on mTOR-regulated Glutamine Uptake and EAAT1-dependent Conversion of Glutamine to Aspartate and Nucleotides. bioRxiv. 2020.
[4] Abrahamsen B, et al. Allosteric modulation of an excitatory amino acid transporter: the subtype-selective inhibitor UCPH-101 exerts sustained inhibition of EAAT1 through an intramonomeric site in the trimerization domain. J Neurosci. 2013 Jan 16;33(3):1068-87. DOI:10.1523/JNEUROSCI.3396-12.2013 |
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| Company Name: |
Energy Chemical
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021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
| Company Name: |
Merck KGaA
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21-20338288 |
| Website: |
www.sigmaaldrich.cn |
| Company Name: |
Abcam Limited
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| Tel: |
021-2070050 400921018 |
| Website: |
www.abcam.cn |
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