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Apafant - ≥98% (HPLC), high purity , CAS No.105219-56-5, Antagonist of PAF receptor

Moligand™
≥98%(HPLC)

CAS#: 105219-56-5
Formula: C₂₂H₂₂ClN₅O₂S
Molecular Weight: 455.96
EC Number: 692-443-7
MDL number: MFCD00865271
PubChem CID: 65889

Item Number

A132597

Grouped product items
SKU	Size	Availability	Price
A132597-1mg	1mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$58.90
A132597-5mg	5mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$147.90
A132597-10mg	10mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$266.90
A132597-25mg	25mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$599.90
A132597-50mg	50mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$1,078.90

Potent PAF receptor antagonist

View related series

PAF receptor Antagonist

Basic Description

Synonyms	Apafant\|105219-56-5\|WEB-2086\|Web 2086\|WEB2086\|WEB 2086BS\|WEB 2086 BS\|CHEMBL280164\|J613NI05SV\|4-(3-(4-(o-Chlorophenyl)-9-methyl-6H-thieno(3,2-f)-s-triazolo(4,3-a)(1,4)diazepin-2-yl)propionyl)morpholine\|DTXSID5048974\|WEB-2086-BS\|3-(4-(2-chlorophenyl)-9-meth
Specifications & Purity	Moligand™, ≥98%(HPLC)
Biochemical and Physiological Mechanisms	Potent, selective platelet-activating factor (PAF) receptor antagonist (Ki= 16.3 nM). Displays anti-inflammatory, antiangiogenic and anticancer activity. Inhibits growth and proliferation of MCF-7 breast cancer cells.
Storage Temp	Store at -20°C
Shipped In	Ice chest + Ice pads
Grade	Moligand™
Action Type	ANTAGONIST
Mechanism of action	Antagonist of PAF receptor
Product Description	Product description Apafant (WEB 2086), a potent platelet-activating factor (PAF) antagonist, inhibits PAF binding to human PAF receptors with a Ki of 9.9 nM.

Associated Targets

CX3CR1 Tchem CX3C chemokine receptor 1 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CYP3A4 Tclin Cytochrome P450 3A4 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

GPR35 Tchem G-protein coupled receptor 35 0 Activities

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BRD4 Tchem Bromodomain-containing protein 4 0 Activities

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CDK2 Tchem Cyclin-dependent kinase 2 0 Activities

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ABCB1 Tchem Multidrug resistance protein 1 0 Activities

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FFAR4 Tchem Free fatty acid receptor 4 0 Activities

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HDAC6 Tclin Histone deacetylase 6 0 Activities

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FPR2 Tchem N-formyl peptide receptor 2 0 Activities

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FGFR3 Tclin Fibroblast growth factor receptor 3 0 Activities

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CSNK1D Tchem Casein kinase I isoform delta 0 Activities

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S1PR1 Tclin Sphingosine 1-phosphate receptor 1 0 Activities

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TRIM24 Tchem Transcription intermediary factor 1-alpha 0 Activities

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ALOX15 Tchem Arachidonate 15-lipoxygenase 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

C5AR1 Tclin C5a anaphylatoxin chemotactic receptor 1 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

BRPF1 Tchem Peregrin 0 Activities

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AURKA Tchem Aurora kinase A 0 Activities

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ADRB2 Tclin Beta-2 adrenergic receptor 0 Activities

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APLNR Tchem Apelin receptor 0 Activities

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ABL1 Tclin Tyrosine-protein kinase ABL1 0 Activities

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ADRA2A Tclin Alpha-2A adrenergic receptor 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ADGRF1 Tbio Adhesion G-protein coupled receptor F1 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

AGTR1 Tclin Type-1 angiotensin II receptor 0 Activities

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GSK3B Tclin Glycogen synthase kinase-3 beta 0 Activities

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GPR119 Tclin Glucose-dependent insulinotropic receptor 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

GLP1R Tclin Glucagon-like peptide 1 receptor 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PTAFR Tchem Platelet-activating factor receptor 3 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

MAPK1 Tchem Mitogen-activated protein kinase 1 0 Activities

Discover Target: MAPK1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Names and Identifiers

IUPAC Name	3-[7-(2-chlorophenyl)-13-methyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.02,6]trideca-2(6),4,7,10,12-pentaen-4-yl]-1-morpholin-4-ylpropan-1-one
INCHI	InChI=1S/C22H22ClN5O2S/c1-14-25-26-19-13-24-21(16-4-2-3-5-18(16)23)17-12-15(31-22(17)28(14)19)6-7-20(29)27-8-10-30-11-9-27/h2-5,12H,6-11,13H2,1H3
InChi Key	JGPJQFOROWSRRS-UHFFFAOYSA-N
Canonical SMILES	CC1=NN=C2N1C3=C(C=C(S3)CCC(=O)N4CCOCC4)C(=NC2)C5=CC=CC=C5Cl
Isomeric SMILES	CC1=NN=C2N1C3=C(C=C(S3)CCC(=O)N4CCOCC4)C(=NC2)C5=CC=CC=C5Cl
WGK Germany	3
Alternate CAS	105219-56-5
PubChem CID	65889
MeSH Entry Terms	3-(4-(2-chlorophenyl)-9-methyl-6H-thieno(3,2-f)(1,2,4)triazolo(4,3-a)(1,4)diazepine-2-yl)-1-(4-morpholinyl)-1-propanone;apafant;triazolodiazepine;WEB 2086;WEB-2086;WEB2086
Molecular Weight	455.96

Solubility

Solvent:DMSO, Max Conc. mg/mL: 45.6, Max Conc. mM: 100; Solvent:ethanol, Max Conc. mg/mL: 45.6, Max Conc. mM: 100 with gentle warming

Sensitivity

Moisture sensitive

Safety and Hazards(GHS)

Pictogram(s)	GHS08
Signal	Warning
Hazard Statements	H361:Suspected of damaging fertility or the unborn child
Precautionary Statements	P280:Wear protective gloves/protective clothing/eye protection/face protection. P405:Store locked up. P501:Dispose of contents/container to ... P203:Obtain, read and follow all safety instructions before use. P318:if exposed or concerned, get medical advice.
WGK Germany	3

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