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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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U274885-1mg | 1mg | In stock | $45.90 | |
U274885-5mg | 5mg | In stock | $189.90 | |
U274885-10mg | 10mg | In stock | $319.90 | |
U274885-25mg | 25mg | In stock | $640.90 | |
U274885-50mg | 50mg | In stock | $1,032.90 | |
U274885-100mg | 100mg | In stock | $1,840.90 |
Selective EAAT1 inhibitor
Synonyms | UCPH-101|1118460-77-7|UCPH 101|UCPH101|2-amino-4-(4-methoxyphenyl)-7-(naphthalen-1-yl)-5-oxo-5,6,7,8-tetrahydro-4H-chromene-3-carbonitrile|2-AMINO-5,6,7,8-TETRAHYDRO-4-(4-METHOXYPHENYL)-7-(NAPHTHALEN-1-YL)-5-OXO-4H-CHROMENE-3-CARBONITRILE|2-amino-4-(4-met |
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Specifications & Purity | ≥98% |
Storage Temp | Store at -20°C,Desiccated |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Inhibitor of Excitatory amino acid transporter 1 |
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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IUPAC Name | 2-amino-4-(4-methoxyphenyl)-7-naphthalen-1-yl-5-oxo-4,6,7,8-tetrahydrochromene-3-carbonitrile |
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INCHI | 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 |
InChi Key | YBMGNDPBARCLFT-UHFFFAOYSA-N |
Canonical SMILES | COC1=CC=C(C=C1)C2C(=C(OC3=C2C(=O)CC(C3)C4=CC=CC5=CC=CC=C54)N)C#N |
Isomeric SMILES | COC1=CC=C(C=C1)C2C(=C(OC3=C2C(=O)CC(C3)C4=CC=CC5=CC=CC=C54)N)C#N |
PubChem CID | 25223366 |
Molecular Weight | 422.48 |
PubChem CID | 25223366 |
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CAS Registry No. | 1118460-77-7 |
ChEMBL Ligand | CHEMBL474133 |
Enter Lot Number to search for COA:
To view the certificate results,please click on a Lot number.For Lot numbers from past orders,please use our order status section
Lot Number | Certificate Type | Date | Item |
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H2224355 | Certificate of Analysis | Jun 07, 2023 | U274885 |
H2224307 | Certificate of Analysis | Jun 07, 2023 | U274885 |
H2224308 | Certificate of Analysis | Jun 07, 2023 | U274885 |
H2224309 | Certificate of Analysis | Jun 07, 2023 | U274885 |
H2224310 | Certificate of Analysis | Jun 07, 2023 | U274885 |
H2224311 | Certificate of Analysis | Jun 07, 2023 | U274885 |
Solubility | Soluble in DMSO to 25 mM |
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1. Jensen AA, Erichsen MN, Nielsen CW, Stensbøl TB, Kehler J, Bunch L. (2009) Discovery of the first selective inhibitor of excitatory amino acid transporter subtype 1.. J Med Chem, 52 (4): (912-5). [PMID:19161278] |
2. Abrahamsen B, Schneider N, Erichsen MN, Huynh TH, Fahlke C, Bunch L, Jensen AA. (2013) 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, 33 (3): (1068-87). [PMID:23325245] |
3. Canul-Tec JC, Assal R, Cirri E, Legrand P, Brier S, Chamot-Rooke J, Reyes N. (2017) Structure and allosteric inhibition of excitatory amino acid transporter 1.. Nature, 544 (7651): (446-451). [PMID:28424515] |
4. Uwechue NM et al.. (2012) Activation of glutamate transport evokes rapid glutamine release from perisynaptic astrocytes.. J Physiol, 590 (Pt 10): (2317-31). [PMID:22411007] |
5. Haym I et al.. (2016) Bioavailability Studies and in vitro Profiling of the Selective Excitatory Amino Acid Transporter Subtype 1 (EAAT1) Inhibitor UCPH-102.. ChemMedChem, [PMID:26797816] |
6. Yang Y & Xu-Friedman MA. (2015) Different pools of glutamate receptors mediate sensitivity to ambient glutamate in the cochlear nucleus.. J Neurophysiol, 113 (10): (3634-45). [PMID:25855696] |
7. Budisantoso T et al.. (2012) Mechanisms underlying signal filtering at a multisynapse contact.. J Neurosci, 32 (7): (2357-76). [PMID:22396411] |
8. Morioka N et al.. (2014) Primary cultures of rat cortical microglia treated with nicotine increases in the expression of excitatory amino acid transporter 1 (GLAST) via the activation of the a7 nicotinic acetylcholine receptor.. Neuroscience, 258 (374-84). [PMID:24300109] |
9. Salvatore MF et al.. (2012) Transient striatal GLT-1 blockade increases EAAC1 expression, glutamate reuptake, and decreases tyrosine hydroxylase phosphorylation at ser(19).. Exp Neurol, 234 (2): (428-36). [PMID:22285253] |