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GSK-189254 , Histamine H3 receptor antagonist, CAS No.720690-73-3, Histamine H3 receptor antagonist

COA COA
In stock
Item Number
G610696
Grouped product items
SKU Size
Availability
 Price Qty
G610696-5mg
5mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$59.90
G610696-10mg
10mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$99.90
G610696-25mg
25mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$199.90
G610696-50mg
50mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$319.90
G610696-100mg
100mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$499.90
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Class A GPCR (4138) H3 receptor Agonist (20)

Basic Description

Synonyms GSK189254A | GSK189254
Specifications & Purity Moligand™, ≥98%
Biochemical and Physiological Mechanisms GSK189254A (GSK189254) is a novel, potent and selective histamine H3 receptor antagonist with pKi values of 9.59-9.90 and 8.51-9.17 for human and rat H3, respectively.
Storage Temp Store at -20°C
Shipped In
Ice chest + Ice pads
This product requires cold chain shipping. Ground and other economy services are not available.
Grade Moligand™
Action Type AGONIST, ANTAGONIST
Mechanism of action Histamine H3 receptor antagonist

Taxonomic Classification

Taxonomy Tree

Kingdom Organic compounds
Superclass Organoheterocyclic compounds
Class Benzazepines
Subclass Not available
Intermediate Tree Nodes Not available
Direct Parent Benzazepines
Alternative Parents Diarylethers  Nicotinamides  Phenol ethers  Azepines  Aralkylamines  Heteroaromatic compounds  Trialkylamines  Secondary carboxylic acid amides  Amino acids and derivatives  Azacyclic compounds  Organic oxides  Hydrocarbon derivatives  
Molecular Framework Aromatic heteropolycyclic compounds
Substituents Benzazepine - Diaryl ether - Nicotinamide - Pyridinecarboxamide - Pyridine carboxylic acid or derivatives - Phenol ether - Azepine - Aralkylamine - Benzenoid - Pyridine - Heteroaromatic compound - Secondary carboxylic acid amide - Amino acid or derivatives - Tertiary aliphatic amine - Tertiary amine - Carboxamide group - Azacycle - Carboxylic acid derivative - Ether - Organic oxide - Amine - Organooxygen compound - Organic oxygen compound - Organic nitrogen compound - Hydrocarbon derivative - Organonitrogen compound - Aromatic heteropolycyclic compound
Description This compound belongs to the class of organic compounds known as benzazepines. These are organic compounds containing a benzene ring fused to an azepine ring (unsaturated seven-membered heterocycle with one nitrogen atom replacing a carbon atom).
External Descriptors Not available

Product Properties

ALogP 3.2

Associated Targets(Human)

HRH3 Tclin Histamine H3 receptor (7 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
HRH2 Tclin Histamine H2 receptor (5428 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HRH1 Tclin Histamine H1 receptor (7573 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
KCNH2 Tclin HERG (29587 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HRH3 Tclin Histamine H3 receptor (10389 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ALB Tchem Serum albumin (2651 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Associated Targets(non-human)

Hrh4 Histamine H4 receptor (388 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Rattus norvegicus (775804 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Brain (1 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Blood (6 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Liver microsome (341 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Mechanisms of Action

Mechanism of Action Action Type target ID Target Name Target Type Target Organism Binding Site Name References

Names and Identifiers

IUPAC Name 6-[(3-cyclobutyl-1,2,4,5-tetrahydro-3-benzazepin-7-yl)oxy]-N-methylpyridine-3-carboxamide
INCHI InChI=1S/C21H25N3O2/c1-22-21(25)17-6-8-20(23-14-17)26-19-7-5-15-9-11-24(18-3-2-4-18)12-10-16(15)13-19/h5-8,13-14,18H,2-4,9-12H2,1H3,(H,22,25)
InChIKey WROHEWWOCPRMIA-UHFFFAOYSA-N
Smiles CNC(=O)C1=CN=C(C=C1)OC2=CC3=C(CCN(CC3)C4CCC4)C=C2
Isomeric SMILES CNC(=O)C1=CN=C(C=C1)OC2=CC3=C(CCN(CC3)C4CCC4)C=C2
Alternate CAS 720690-73-3
PubChem CID 9798547
MeSH Entry Terms 6-((3-cyclobutyl-2,3,4,5-tetrahydro-1H-3-benzazepin-7-yl)oxy)-N-methyl-3-pyridinecarboxamide;GSK 189254;GSK-189254;GSK189254
Molecular Weight 351.44

Certificates（CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:

Chemical and Physical Properties

Solubility DMSO: 24 mg/mL (68.29 mM), Sonication is recommended.
Molecular Weight 351.400 g/mol
XLogP3 3.200
Hydrogen Bond Donor Count 1
Hydrogen Bond Acceptor Count 4
Rotatable Bond Count 4
Exact Mass 351.195 Da
Monoisotopic Mass 351.195 Da
Topological Polar Surface Area 54.500 Ų
Heavy Atom Count 26
Formal Charge 0
Complexity 482.000
Isotope Atom Count 0
Defined Atom Stereocenter Count 0
Undefined Atom Stereocenter Count 0
Defined Bond Stereocenter Count 0
Undefined Bond Stereocenter Count 0
The total count of all stereochemical bonds 0
Covalently-Bonded Unit Count 1

Solution Calculators

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Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.
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