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NBI-74330

Chemical Structure : NBI-74330

CAS No.: 855527-92-3

NBI-74330 (NBI 74330, VUF10472)

Catalog No.: PC-73268Not For Human Use, Lab Use Only.

NBI-74330 is a potent, selective CXC chemokine receptor 3 (CXCR3) antagonist, inhibits [(125)I]CXCL10 and [(125)I]CXCL11 specific binding with Ki of 1.5 and 2.3 nM, respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

NBI-74330 (VUF10472) is a potent, selective CXC chemokine receptor 3 (CXCR3) antagonist, inhibits [(125)I]CXCL10 and [(125)I]CXCL11 specific binding with Ki of 1.5 and 2.3 nM, respectively.
NBI-74330 exhibited specific inhibition of functional responses mediated by CXCR3, such as ligand-induced guanosine 5'-O-(3-[(35)S]thio)triphosphate ([(35)S]GTPgammaS) binding, calcium mobilization, and cellular chemotaxis (IC50=7-18 nM).
NBI-74330 showed no significant inhibition of chemotactic responses to other chemokines and did not inhibit radioligand binding to a panel of nonchemokine G-protein coupled receptors.
NBI-74330 block CXCR3-mediated signaling in peritonitis and diet-induced atherosclerosis, attenuates atherosclerotic plaque formation in LDL receptor-deficient mice。

Physicochemical Properties

M.Wt 605.58
Formula C32H27F4N5O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-1R-[3-(4-ethoxy-phenyl)-4-oxo-3,4-dihydro-pyrido[2,3-d]pyrimidin-2-yl]-ethyl-N-pyridin-3-ylmethyl-2-(4-fluoro-3-trifluoromethyl-phenyl)-acetamide

References

1. Heise CE, et al. J Pharmacol Exp Ther. 2005 Jun;313(3):1263-71.

2. Jopling LA, et al. Br J Pharmacol. 2007 Dec;152(8):1260-71.

3. van Wanrooij EJ, et al. Arterioscler Thromb Vasc Biol. 2008 Feb;28(2):251-7.

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