Fluperlapine - ≥95%, high purity , CAS No.67121-76-0, Antagonist of 5-HT 6 receptor;Antagonist of 5-HT 7 receptor

Item Number
F336050
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F336050-1mg
1mg
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$47.90
F336050-5mg
5mg
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$215.90
F336050-10mg
10mg
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$380.90

an agonist of the serotonin 5-HT6/5-HT7 receptors

Basic Description

SynonymsGTPL279 | HMS2090H12 | 3-Fluoro-6-(4-methyl-piperazin-1-yl)-11H-dibenzo[b,e]azepine | L000256 | Tox21_111780_1 | BPBio1_001099 | FLUPERLAPINE [MART.] | HMS2052M07 | FLUPERLAPINE | PDSP1_000472 | DTXCID0026123 | NB-106689 | SCHEMBL142558 | C10967 | NCGC001
Specifications & PurityMoligand™, ≥95%
Storage TempRoom temperature
Shipped InNormal
GradeMoligand™
Action TypeANTAGONIST
Mechanism of actionAntagonist of 5-HT 6 receptor;Antagonist of 5-HT 7 receptor
Product Description

Fluperlapine is an agonist of the SR-6/SR-7 (serotonin 5-HT|6|/5-HT|7|receptors). Agonism of the 5-HT|6|/5-HT|7|receptors by Fluperlapine has been correlated to sedative effects. Fluperlapine is described to function similarly to Clozapine , and Fluperlapine is also described to be relatively resistant to chemical and biochemical oxidation as compared to Clozapine.

Product Properties

pKapKₐ: 7.46 (Predicted)
Ki DataSerotonin 2a receptor: Ki= 3.8 nM (Rattus norvegicus); Serotonin 2b receptor: Ki= 3.8 nM (Rattus norvegicus); Serotonin 2c receptor: Ki= 3.8 nM (Rattus norvegicus); Muscarinic acetylcholine receptor: Ki= 25 nM (Rattus norvegicus)

Associated Targets(Human)

HTR7 Tclin 5-hydroxytryptamine receptor 7 (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
HTR6 Tchem 5-hydroxytryptamine receptor 6 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
DRD2 Tclin Dopamine D2 receptor (23596 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
DRD1 Tclin Dopamine D1 receptor (9720 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
TDP1 Tchem Tyrosyl-DNA phosphodiesterase 1 (345557 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Mapk1 MAP kinase ERK2 (650 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Pseudomonas aeruginosa (123386 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Klebsiella pneumoniae (43867 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Staphylococcus aureus (210822 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Acinetobacter baumannii (41033 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Escherichia coli (133304 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Saccharomyces cerevisiae (19171 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Cryptococcus neoformans (21258 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Candida albicans (78123 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Trpa1 Transient receptor potential cation channel subfamily A member 1 (1003 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Chrm1 Muscarinic acetylcholine receptor (3770 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Htr2b Serotonin 2 (5-HT2) receptor (2078 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Drd1 Dopamine receptors; D1 & D2 (258 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Drd2 Dopamine D2 receptor/Serotonin 2 (5-HT2) receptor (132 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

IUPAC Name 3-fluoro-6-(4-methylpiperazin-1-yl)-11H-benzo[c][1]benzazepine
INCHI InChI=1S/C19H20FN3/c1-22-8-10-23(11-9-22)19-17-5-3-2-4-14(17)12-15-6-7-16(20)13-18(15)21-19/h2-7,13H,8-12H2,1H3
InChi Key OBWGMKKHCLHVIE-UHFFFAOYSA-N
Canonical SMILES CN1CCN(CC1)C2=NC3=C(CC4=CC=CC=C42)C=CC(=C3)F
Isomeric SMILES CN1CCN(CC1)C2=NC3=C(CC4=CC=CC=C42)C=CC(=C3)F
PubChem CID 49381
Molecular Weight 309.4

Certificates

Certificate of Analysis(COA)

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Chemical and Physical Properties

SolubilitySoluble in DMSO (10 mg/ml), and ethanol (20 mg/ml).
Refractive Indexn20D1.64 (Predicted)
Boil Point(°C)~438.74° C at 760 mmHg (Predicted)
Melt Point(°C)~18-20° C

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