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Chemical Structure : NBI-74330
CAS No.: 855527-92-3
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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $158 | In stock | |
| 10 mg | $248 | In stock | |
| 25 mg | $398 | In stock | |
| 50 mg | Get quote | ||
| 100 mg | Get quote |
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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。
| M.Wt | 605.58 | |
| Formula | C32H27F4N5O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| 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 |
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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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