(±)-NBI 74330

Name: (±)-NBI 74330
Brand: Tocris Bioscience
SKU: 4528

Tocris Bioscience, part of Bio-Techne | Catalog # 4528

Citations (12)

COA / SDS

Potent and selective CXCR3 antagonist

Key Product Details

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)
Molecular Weight:	605.58

View Full Technical Details for (±)-NBI 74330

Technical Data
Citations

Biological Activity for (±)-NBI 74330

(±)-NBI 74330 is a potent and selective CXCR3 antagonist; potently inhibits ¹²⁵I-CXCL10 binding to CXCR3 (pK_i = 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 for (±)-NBI 74330

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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	3.30 mL	16.51 mL	33.03 mL
2.5 mM	0.66 mL	3.30 mL	6.61 mL
5 mM	0.33 mL	1.65 mL	3.30 mL
25 mM	0.07 mL	0.33 mL	0.66 mL

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References for (±)-NBI 74330

References are publications that support the biological activity of the product.

Verzijl Noncompetitive antagonism and inverse agonism as mechanism of action of nonpeptidergic antagonists at primate and rodent CXCR3 chemokine receptors. J.Pharmacol.Exp.Ther. 2008 PMID: 18270317
Heise Pharmacological characterization of CXC chemokine receptor 3 ligands and a small molecule antagonist. J.Pharmacol.Exp.Ther. 2005 PMID: 15761110
Storelli 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. 2007 PMID: 17562560