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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% (HPLC)
Biological Activity for (±)-NBI 74330
(±)-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.
Compound Libraries for (±)-NBI 74330
(±)-NBI 74330 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.
Technical Data for (±)-NBI 74330
| M. Wt | 605.58 |
| Formula | C32H27F4N5O3 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 473722-68-8 |
| PubChem ID | 10167713 |
| InChI Key | XMRGQUDUVGRCBS-UHFFFAOYSA-N |
| Smiles | CCOC(C=C3)=CC=C3N2C(C1=CC=CN=C1N=C2C(N(CC4=CC=CN=C4)C(CC5=CC(C(F)(F)F)=C(F)C=C5)=O)C)=O |
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.
Solubility Data for (±)-NBI 74330
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 30.28 | 50 |
Preparing Stock Solutions for (±)-NBI 74330
The following data is based on the product molecular weight 605.58. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.5 mM | 3.3 mL | 16.51 mL | 33.03 mL |
| 2.5 mM | 0.66 mL | 3.3 mL | 6.61 mL |
| 5 mM | 0.33 mL | 1.65 mL | 3.3 mL |
| 25 mM | 0.07 mL | 0.33 mL | 0.66 mL |
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Product Datasheets for (±)-NBI 74330
References for (±)-NBI 74330
References are publications that support the biological activity of the product.
Storelli et al (2007) Synthesis and structure-activity relationships of 3H-quinazolin-4-ones and 3H-pyrido[2,3-d]pyrimidin-4-ones as CXCR3 receptor antagonists. Arch.Pharm. 340 281 PMID: 17562560
Verzijl et al (2008) Noncompetitive antagonism and inverse agonism as mechanism of action of nonpeptidergic antagonists at primate and rodent CXCR3 chemokine receptors. J.Pharmacol.Exp.Ther. 325 544 PMID: 18270317
Heise et al (2005) Pharmacological characterization of CXC chemokine receptor 3 ligands and a small molecule antagonist. J.Pharmacol.Exp.Ther. 313 1263 PMID: 15761110
If you know of a relevant reference for (±)-NBI 74330, please let us know.
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Keywords: (±)-NBI 74330, (±)-NBI 74330 supplier, VUF10472, (±)-NBI74330, potent, selective, CXCR3, antagonists, chemokines, (±)-NBI_74330, Chemokine, CXC, Receptors, 4528, Tocris Bioscience
1 Citation for (±)-NBI 74330
Citations are publications that use Tocris products. Selected citations for (±)-NBI 74330 include:
Piotrowska et al (2018) Pharmacological blockade of CXCR3 by (±)-NBI-74330 reduces neuropathic pain and enhances opioid effectiveness - Evidence from in vivo and in vitro studies. Biochim.Biophys.Acta 1864 3418 PMID: 30076959
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