(±)-NBI 74330

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Cat.No. 4528 - (±)-NBI 74330 | C32H27F4N5O3 | CAS No. 473722-68-8
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)
Datasheet
Citations
Literature

Biological Activity

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 (Cat. No. 4487).

Compound Libraries

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Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 30.28 50

Preparing Stock Solutions

The following data is based on the product molecular weight 605.58. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.65 mL 8.26 mL 16.51 mL
5 mM 0.33 mL 1.65 mL 3.3 mL
10 mM 0.17 mL 0.83 mL 1.65 mL
50 mM 0.03 mL 0.17 mL 0.33 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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


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Citations for (±)-NBI 74330

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