193542-65-3
Chemical Structure
BX-513
Synonym(s): VUF 2274
- CAS No.: 193542-65-3
- Formula:C28H29ClN2O
- Molecular Weight:445.00
IUPAC Name: 5-(4-(4-chlorophenyl)-4-hydroxypiperidin-1-yl)-2,2-diphenylpentanenitrile
InChIKey: MEEJEEVTIVAOJP-UHFFFAOYSA-N
SMILES: N#CC(C=1C=CC=CC1)(C=2C=CC=CC2)CCCN3CCC(O)(C4=CC=C(Cl)C=C4)CC3
Biological Activity: BX-513 (VUF2274) is a CCR1 antagonist that inhibits chemokine binding and blocks US28 signaling. BX-513 inhibits human CCR1 with a Ki of 40 nM. BX-513 blocks CCL3-mediated signaling/chemotaxis, CCR1-mediated chemokine signaling, calcium mobilization, extracellular acidification, and US28-mediated HIV entry, with an IC50 of 4.9 μM. BX-513 can be used for research on hcmv infection[1][2][3].
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BX-513 | BX-513 (VUF2274) is a CCR1 antagonist that inhibits chemokine binding and blocks US28 signaling. BX-513 inhibits human CCR1 with a Ki of 40 nM. BX-513 blocks CCL3-mediated signaling/chemotaxis, CCR1-mediated chemokine signaling, calcium mobilization, extracellular acidification, and US28-mediated HIV entry, with an IC50 of 4.9 μM. BX-513 can be used for research on hcmv infection. | |||||||||||||||||||||
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References
- [1]. Hulshof JW, et al. Synthesis and pharmacological characterization of novel inverse agonists acting on the viral-encoded chemokine receptor US28. Bioorganic & medicinal chemistry. 2006 Nov 01;14(21):7213-30. [Content Brief]
- [2]. Horuk R, et al. BX471: a CCR1 antagonist with anti-inflammatory activity in man. Mini reviews in medicinal chemistry. 2005 Sep;5(9):791-804. [Content Brief]
- [3]. Onuffer J, et al. Structure function differences in nonpeptide CCR1 antagonists for human and mouse CCR1. The Journal of Immunology. 2003 Feb;170(4):1910-6.