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(±)-NBI 74330

Catalog #: 4528
1 Citation Datasheet
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(±)-NBI 74330 | CAS No. 473722-68-8 | Chemokine Receptor Antagonists
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Description: Potent and selective CXCR3 antagonist

Chemical Name: N-1-[(3-4(-Ethoxyphenyl)-3,4-dihydro-4-oxopyrido[2,3-d]pyrimidin-2-yl]ethyl]-4-fluoro-N-(3-pyridinylmethyl)-3-(trifluoromethyl)benzeneacetamide

Purity: ≥98%

Product Details
Citations (1)
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Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

(±)-NBI 74330 is a potent and selective CXCR3 antagonist; potently inhibits 125I-CXCL10 binding to CXCR3 (pKi = 8.13). Inhibits calcium mobilization in response to CXCL11 and CXCL10 in RBL cells. Exhibits no significant effect on chemotaxis induced by CXCR4 or CCR7. Displays a five-fold greater affinity for CXCR3 than (±)-AMG 487.

This product is racemic.

Technical Data

M.Wt:
605.58
Formula:
C32H27F4N5O3
Solubility:
Soluble to 50 mM in DMSO
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
473722-68-8

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Other Product-Specific Information:
  • This compound is racemic

Background References

  1. Osteoblasts secrete Cxcl9 to regulate angiogenesis in bone

    Nat Commun, 2016;7(0):13885.
  2. Synthesis and structure-activity relationships of 3H-quinazolin-4-ones and 3H-pyrido[2,3-d]pyrimidin-4-ones as CXCR3 receptor antagonists.
    Storelli et al.
    Arch.Pharm., 2007;340:281
  3. Noncompetitive antagonism and inverse agonism as mechanism of action of nonpeptidergic antagonists at primate and rodent CXCR3 chemokine receptors.
    Verzijl et al.
    J.Pharmacol.Exp.Ther., 2008;325:544
  4. Pharmacological characterization of CXC chemokine receptor 3 ligands and a small molecule antagonist.
    Heise et al.
    J.Pharmacol.Exp.Ther., 2005;313:1263
  5. The atypical chemokine receptor 3 interacts with Connexin 43 inhibiting astrocytic gap junctional intercellular communication
    A Fumagalli, J Heuninck, A Pizzoccaro, E Moutin, J Koenen, M Séveno, T Durroux, MP Junier, G Schlecht-L, F Bachelerie, D Schütz, R Stumm, MJ Smit, NC Guérineau, S Chaumont-D, P Marin
    Nat Commun, 2020;11(1):4855.

Product Datasheets

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Citation for (±)-NBI 74330

The citations listed below are publications that use Tocris products. Selected citations for (±)-NBI 74330 include:

1 Citation: Showing 1 - 1

  1. Pharmacological blockade of CXCR3 by (�)-NBI-74330 reduces neuropathic pain and enhances opioid effectiveness - Evidence from in vivo and in vitro studies.
    Authors: Piotrowska Et al.
    Biochim.Biophys.Acta  2018;1864:3418

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