LAU463 , CAS No.L611460, Allosteric modulator of GABA A receptor α6 subunit

Item Number
L611460
Grouped product items
SKUSizeAvailabilityPrice Qty
L611460-5mg
5mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$570.90
L611460-25mg
25mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$2,000.90

Basic Description

SynonymsLAU463 | CHEMBL4092332 | SCHEMBL18285404 | GTPL12405 | DTXSID901150239 | compound 8n [PMID: 29481759] | 7-Bromo-2,5-dihydro-2-(4-methoxyphenyl)-3H-pyrazolo[4,3-c]quinolin-3-one | 2055050-88-7
Specifications & PurityMoligand™
GradeMoligand™
Action TypeALLOSTERIC MODULATOR
Mechanism of actionAllosteric modulator of GABA A receptor α6 subunit

Associated Targets(Human)

GABRA6 Tclin Gamma-aminobutyric acid receptor subunit alpha-6 (0 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
KCNH2 Tclin HERG (29587 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Liver (3974 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
GABRG2 Tclin GABA-A receptor; alpha-3/beta-3/gamma-2 (1250 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
GABRA1 Tclin GABA-A receptor; alpha-1/beta-3/gamma-2 (1565 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
GABRG2 Tclin GABA-A receptor; alpha-5/beta-3/gamma-2 (1334 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
GABRG2 Tclin GABA-A receptor; alpha-2/beta-3/gamma-2 (949 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
GABRG2 Tclin GABA-A receptor; alpha-6/beta-3/gamma-2 (367 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
GABRG2 Tclin GABA A receptor alpha-4/beta-3/gamma-2 (109 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Mus musculus (284745 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Gabrg2 Gamma-aminobutyric acid receptor subunit alpha-6/beta-3/gamma-2 (184 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Gabrg2 Gamma-aminobutyric acid receptor subunit alpha-1/beta-3/gamma-2 (2 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Gabrg2 Gamma-aminobutyric acid receptor subunit alpha-1/alpha-6/beta-3/gamma-2 (42 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

INCHI InChI=1S/C17H12BrN3O2/c1-23-12-5-3-11(4-6-12)21-17(22)14-9-19-15-8-10(18)2-7-13(15)16(14)20-21/h2-9,19H,1H3
InChi Key CAJJWNTVLDPILI-UHFFFAOYSA-N
Canonical SMILES COC1=CC=C(C=C1)N2N=C3C(=CNC4=C3C=CC(Br)=C4)C2=O
Isomeric SMILES COC1=CC=C(C=C1)N2C(=O)C3=CN=C4C=C(C=CC4=C3N2)Br
PubChem CID 124111379

Certificates

Certificate of Analysis(COA)

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Related Documents

References

1. Knutson DE, Kodali R, Divović B, Treven M, Stephen MR, Zahn NM, Dobričić V, Huber AT, Meirelles MA, Verma RS et al..  (2018)  Design and Synthesis of Novel Deuterated Ligands Functionally Selective for the γ-Aminobutyric Acid Type A Receptor (GABAAR) α6 Subtype with Improved Metabolic Stability and Enhanced Bioavailability..  J Med Chem,  61  (6): (2422-2446).  [PMID:29481759]
2. Varagic Z, Wimmer L, Schnürch M, Mihovilovic MD, Huang S, Rallapalli S, Cook JM, Mirheydari P, Ecker GF, Sieghart W et al..  (2013)  Identification of novel positive allosteric modulators and null modulators at the GABAA receptor α+β- interface..  Br J Pharmacol,  169  (2): (371-83).  [PMID:23472852]

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