A CXCR3 antagonist
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AMG 487

Item No. 28416

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[(1R)-1-[3-(4-ethoxyphenyl)-3,4-dihydro-4-oxopyrido[2,3-d]pyrimidin-2-yl]ethyl]-N-(3-pyridinylmethyl)-4-(trifluoromethoxy)-benzeneacetamide
CAS Number
473719-41-4
Molecular Formula
C32H28F3N5O4
Formula Weight
603.6
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 60 mg/ml
λmax
269 nm
SMILES
O=C(N([C@@H](C1=NC(N=CC=C2)=C2C(N1C3=CC=C(OCC)C=C3)=O)C)CC4=CN=CC=C4)CC5=CC=C(OC(F)(F)F)C=C5
InChi Code
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $63

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    5 mg

    $197

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    10 mg

    $333

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    25 mg

    $753

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    Cayman Chemical
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    OBESITY RESEARCH SOLUTIONS
    Product Description

    AMG 487 is a chemokine (C-X-C motif) receptor 3 (CXCR3) antagonist (IC50 = 8.2 nM in a radioligand binding assay).1 It inhibits cell migration induced by chemokine (C-X-C motif) ligand 10 (CXCL10), CXCL11, and CXCL9 (IC50s = 8, 15, and 36 nM, respectively). In vivo, AMG 487 (3 mg/kg) inhibits bronchoalveolar lavage fluid (BALF) cell infiltration in a mouse model of bleomycin-induced cellular recruitment. It reduces the number of lung metastases in the K7M2 and Saos-LM7 osteosarcoma mouse xenograft models.2 AMG 487 (5 mg/kg) also restores mitochondrial function and inhibits mitochondrial-dependent hepatocellular apoptosis in a mouse model of non-alcoholic steatohepatitis (NASH).3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Johnson, M., Li, A.-R., Liu, J., et al. Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3. Bioor. Med. Chem. 17(12), 3339-3343 (2007).

    2. Pradelli, E., Karimdjee-Soilihi, B., Michiels, J.F., et al. Antagonism of chemokine receptor CXCR3 inhibits osteosarcoma metastasis to lungs. Int. J. Cancer 125(11), 2586-2594 (2009).

    3. Du, J., Zhang, X., Han, J., et al. Pro-inflammatory CXCR3 impairs mitochondrial function in experimental non-alcoholic steatohepatitis. Theranostics 7(17), 4192-4203 (2017).