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A 841720 - ≥98%, high purity , CAS No.869802-58-4, Allosteric modulator of mGlu 1 receptor

Item Number
A345272
Grouped product items
SKUSizeAvailabilityPrice Qty
A345272-10mg
10mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$160.90
A345272-50mg
50mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$676.90

a potent & non-competitive mGluR-1 antagonist

Basic Description

SynonymsBDBM50177080 | 9-dimethylamino-3-(N-hexamethyleneiminyl)-3H-5-thia-1,3,6-triazafluoren-4-one | 9-(DIMETHYLAMINO)-3-(HEXAHYDRO-1H-AZEPIN-1-YL)PYRIDO[3' ,2':4,5]THIENO[3,2-D]PYRIMIDIN-4(3H)-ONE | DTXSID10236030 | A-440 | UNII-U8C5C9D65S | AKOS024457407 | A
Specifications & PurityMoligand™, ≥98%
Storage TempRoom temperature
Shipped InNormal
GradeMoligand™
Action TypeALLOSTERIC MODULATOR
Mechanism of actionAllosteric modulator of mGlu 1 receptor
Product Description

A 841720 is a potent, non-competitive mGluR-1 antagonist that displays 34-fold selectivity over mGluR-5 (IC|50|values are 10 and 342 nM respectively). A 841720 displays no significant activity at a range of other GPCRs, ion channels and transporters. This compound also exhibits analgesic effects, decreases mechanical allodynia in models of neuropathic pain, and impairs cognitive function.

Associated Targets(Human)

GRM1 Tchem Metabotropic glutamate receptor 1 (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
ABL1 Tclin Tyrosine-protein kinase ABL (18331 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ADRB2 Tclin Beta-2 adrenergic receptor (11824 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ADRA2A Tclin Alpha-2a adrenergic receptor (9450 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
AGTR1 Tclin Type-1 angiotensin II receptor (5176 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
GSK3B Tclin Glycogen synthase kinase-3 beta (11785 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CSNK1D Tchem Casein kinase I delta (4546 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
GRM1 Tchem Metabotropic glutamate receptor 1 (2309 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
GRM5 Tchem Metabotropic glutamate receptor 5 (5733 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
S1PR1 Tclin Sphingosine 1-phosphate receptor Edg-1 (5806 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CDK2 Tchem Cyclin-dependent kinase 2 (9050 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
GLP1R Tclin Glucagon-like peptide 1 receptor (111429 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
C5AR1 Tclin C5a anaphylatoxin chemotactic receptor (2677 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
AURKA Tchem Serine/threonine-protein kinase Aurora-A (10240 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
U2OS (164939 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CX3CR1 Tchem C-X3-C chemokine receptor 1 (1686 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
FPR2 Tchem Lipoxin A4 receptor (3472 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
FFAR4 Tchem G-protein coupled receptor 120 (2999 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
BRD4 Tchem Bromodomain-containing protein 4 (13122 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
GPR35 Tchem G-protein coupled receptor 35 (2643 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
TRIM24 Tchem Transcription intermediary factor 1-alpha (2087 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
BRPF1 Tchem Peregrin (2217 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HEK-293T (167025 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Aplnr Apelin receptor (201 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Mapk1 MAP kinase ERK2 (650 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Fgfr3 Fibroblast growth factor receptor 3 (21 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Rattus norvegicus (775804 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Gpr119 Glucose-dependent insulinotropic receptor (270 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences
Tyrosine-protein kinase ABL inhibitorINHIBITORALA1862Tyrosine-protein kinase ABLSINGLE PROTEINHomo sapiens

DailyMed: [1]


Tyrosine-protein kinase ABL inhibitorINHIBITORALA1862Tyrosine-protein kinase ABLSINGLE PROTEINHomo sapiens

DailyMed: [1]


Tyrosine-protein kinase ABL inhibitorINHIBITORALA1862Tyrosine-protein kinase ABLSINGLE PROTEINHomo sapiens

Expert: [1]


Tyrosine-protein kinase ABL inhibitorINHIBITORALA1862Tyrosine-protein kinase ABLSINGLE PROTEINHomo sapiens

Expert: [1]


FDA: [1]


Tyrosine-protein kinase ABL inhibitorINHIBITORALA1862Tyrosine-protein kinase ABLSINGLE PROTEINHomo sapiens

DailyMed: [1]


Wikipedia: [1]


Tyrosine-protein kinase ABL inhibitorINHIBITORALA1862Tyrosine-protein kinase ABLSINGLE PROTEINHomo sapiens

Other: [1] , [2]


Tyrosine-protein kinase ABL inhibitorINHIBITORALA1862Tyrosine-protein kinase ABLSINGLE PROTEINHomo sapiens

ClinicalTrials: [1]


PubMed: [1]


Tyrosine-protein kinase ABL inhibitorINHIBITORALA1862Tyrosine-protein kinase ABLSINGLE PROTEINHomo sapiens

PubMed: [1] , [2]


Tyrosine-protein kinase ABL inhibitorINHIBITORALA1862Tyrosine-protein kinase ABLSINGLE PROTEINHomo sapiens

DOI: [1]


Other: [1]


PubMed: [1]


Tyrosine-protein kinase ABL inhibitorINHIBITORALA1862Tyrosine-protein kinase ABLSINGLE PROTEINHomo sapiens

PubMed: [1]


Names and Identifiers

IUPAC Name 5-(azepan-1-yl)-13-(dimethylamino)-8-thia-3,5,10-triazatricyclo[7.4.0.02,7]trideca-1(13),2(7),3,9,11-pentaen-6-one
INCHI InChI=1S/C17H21N5OS/c1-20(2)12-7-8-18-16-13(12)14-15(24-16)17(23)22(11-19-14)21-9-5-3-4-6-10-21/h7-8,11H,3-6,9-10H2,1-2H3
InChi Key GYWGXEGOXODOQU-UHFFFAOYSA-N
Canonical SMILES CN(C)C1=C2C3=C(C(=O)N(C=N3)N4CCCCCC4)SC2=NC=C1
Isomeric SMILES CN(C)C1=C2C3=C(C(=O)N(C=N3)N4CCCCCC4)SC2=NC=C1
PubChem CID 11559235
Molecular Weight 343.45

Certificates

C of A & Other Certificates

Chemical and Physical Properties

SolubilitySoluble to 50 mM in DMSO and to 50 mM in Ethanol

Related Documents

Solution Calculators