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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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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
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 |
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Specifications & Purity | ≥98% |
Biochemical and Physiological Mechanisms | 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. |
Storage Temp | Store at -20°C |
Shipped In | Ice 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 |
ALogP | 6.334 |
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Rotatable Bond | 11 |
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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 |
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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 |
Enter Lot Number to search for COA:
To view the certificate results,please click on a Lot number.For Lot numbers from past orders,please use our order status section
Lot Number | Certificate Type | Date | Item |
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G2403127 | Certificate of Analysis | May 27, 2024 | A414114 |
G2403128 | Certificate of Analysis | May 27, 2024 | A414114 |
K2209190 | Certificate of Analysis | Jun 27, 2022 | A414114 |
K2209191 | Certificate of Analysis | Jun 27, 2022 | A414114 |
K2209192 | Certificate of Analysis | Jun 27, 2022 | A414114 |
K2209193 | Certificate of Analysis | Jun 27, 2022 | A414114 |
K2209195 | Certificate of Analysis | Jun 27, 2022 | A414114 |
K2219198 | Certificate of Analysis | Jun 27, 2022 | A414114 |
DMSO(mg / mL) Max Solubility | 100 |
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DMSO(mM) Max Solubility | 165.675375668914 |
Water(mg / mL) Max Solubility | <1 |
Starting at $241.90