AMG 487 - 98%, high purity , CAS No.473719-41-4

  • ≥98%
Item Number
A414114
Grouped product items
SKUSizeAvailabilityPrice Qty
A414114-1mg
1mg
In stock
$13.90
A414114-5mg
5mg
In stock
$46.90
A414114-10mg
10mg
In stock
$84.90
A414114-25mg
25mg
In stock
$188.90
A414114-50mg
50mg
In stock
$340.90
A414114-100mg
100mg
In stock
$612.90

CXCR Antagonists

Basic Description

Synonyms(R)-N-(1-(3-(4-ethoxyphenyl)-4-oxo-3,4-dihydropyrido[2,3-d]pyrimidin-2-yl)ethyl)-N-(pyridin-3-ylmethyl)-2-(4-(trifluoromethoxy)phenyl)acetamide | AMG487 | AMG-487 | 355CGR2CBL | Benzeneacetamide, N-((1R)-1-(3-(4-ethoxyphenyl)-3,4-dihydro-4-oxopyrido(2,3-d
Specifications & Purity≥98%
Biochemical and Physiological MechanismsAMG 487 is an orally active and selective CXC chemokine receptor 3 (CXCR3) antagonist that inhibits the binding of IP-10 (CXCL10) and ITAC (CXCL11) to CXCR3 with IC50 of 8.0 nM and 8.2 nM, respectively.
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
Product Description

Information

AMG 487 AMG 487 is an orally active and selective CXC chemokine receptor 3 (CXCR3) antagonist that inhibits the binding of IP-10 (CXCL10) and ITAC (CXCL11) to CXCR3 with IC50 of 8.0 nM and 8.2 nM, respectively.


Targets

CXCR3-CXCL10 (Cell-free assay); CXCR3-CXCL11 (Cell-free assay) 8.0 nM; 8.2 nM


In vitro

AMG487 is the targeted blocker of chemokine receptor CXCR3 and improves inflammatory symptoms by blocking the inflammatory cycle. AMG487 significantly affects DC maturity in vitro and function leading to impaired T cell activation, inducing DCs to have characteristics similar to tolerogenic DCs. AMG487 may directly play an immunomodulatory role during DC development and functional shaping.


In vivo

AMG487 exhibits the antiarthritic effects in DBA/1J mice bearing collageninduced arthritis (CIA).


Cell Research(from reference)

Cell lines:Murine bone marrow-derived DCs (BMDCs) 

Concentrations:3 μM, 15 μM, 30 μM, 60 μM 

Incubation Time:over 6 days 

Product Properties

ALogP6.334
Rotatable Bond11

Associated Targets(Human)

CXCR3 Tchem C-X-C chemokine receptor type 3 (17 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
CHRM2 Tclin Muscarinic acetylcholine receptor M2 (10671 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CHRM1 Tclin Muscarinic acetylcholine receptor M1 (12690 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CHRM3 Tclin Muscarinic acetylcholine receptor M3 (7750 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CXCR3 Tchem C-X-C chemokine receptor type 3 (2736 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP3A4 Tclin Cytochrome P450 3A4 (53859 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Hdac6 Histone deacetylase 6 (222 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Canis familiaris (36305 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Mus musculus (284745 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Rattus norvegicus (775804 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Cynomolgus monkey (4946 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Blood (6 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SARS-CoV-2 (38078 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Names and Identifiers

IUPAC Name N-[(1R)-1-[3-(4-ethoxyphenyl)-4-oxopyrido[2,3-d]pyrimidin-2-yl]ethyl]-N-(pyridin-3-ylmethyl)-2-[4-(trifluoromethoxy)phenyl]acetamide
INCHI InChI=1S/C32H28F3N5O4/c1-3-43-25-14-10-24(11-15-25)40-30(38-29-27(31(40)42)7-5-17-37-29)21(2)39(20-23-6-4-16-36-19-23)28(41)18-22-8-12-26(13-9-22)44-32(33,34)35/h4-17,19,21H,3,18,20H2,1-2H3/t21-/m1/s1
InChi Key WQTKNBPCJKRYPA-OAQYLSRUSA-N
Canonical SMILES CCOC1=CC=C(C=C1)N2C(=O)C3=C(N=CC=C3)N=C2C(C)N(CC4=CN=CC=C4)C(=O)CC5=CC=C(C=C5)OC(F)(F)F
Isomeric SMILES CCOC1=CC=C(C=C1)N2C(=O)C3=C(N=CC=C3)N=C2[C@@H](C)N(CC4=CN=CC=C4)C(=O)CC5=CC=C(C=C5)OC(F)(F)F
PubChem CID 24957182
Molecular Weight 603.59

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Certificate of Analysis(COA)

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8 results found

Lot NumberCertificate TypeDateItem
G2403127Certificate of AnalysisMay 27, 2024 A414114
G2403128Certificate of AnalysisMay 27, 2024 A414114
K2209190Certificate of AnalysisJun 27, 2022 A414114
K2209191Certificate of AnalysisJun 27, 2022 A414114
K2209192Certificate of AnalysisJun 27, 2022 A414114
K2209193Certificate of AnalysisJun 27, 2022 A414114
K2209195Certificate of AnalysisJun 27, 2022 A414114
K2219198Certificate of AnalysisJun 27, 2022 A414114

Chemical and Physical Properties

DMSO(mg / mL) Max Solubility100
DMSO(mM) Max Solubility165.675375668914
Water(mg / mL) Max Solubility<1

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