370893-06-4
Chemical Structure
Ancriviroc
Synonym(s): SCH-351125
- CAS 番号: 370893-06-4
- Formula:C28H37BrN4O3
- Molecular Weight:557.52
IUPAC Name: (Z)-3-(4-((4-bromophenyl)(ethoxyimino)methyl)-4'-methyl-[1,4'-bipiperidine]-1'-carbonyl)-2,4-dimethylpyridine 1-oxide
InChIKey: ZGDKVKUWTCGYOA-URGPHPNLSA-N
SMILES: CCO/N=C(C1=CC=C(C=C1)Br)/C2CCN(C3(CCN(CC3)C(C4=C([N+]([O-])=CC=C4C)C)=O)C)CC2
Biological Activity: Ancriviroc (SCH-351125) is an orally active CCR5 antagonist with an IC50 value of 13 nM against hCCR5. Ancriviroc specifically binds to hCCR5, blocks ligand-induced signal transduction, calcium influx, GTPγS binding, chemotaxis, ligand binding, and HIV-1 entry, induces conformational changes in CCR5, and inhibits infection and replication of R5-tropic HIV-1[1][2].
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Ancriviroc | Ancriviroc (SCH-351125) is an orally active CCR5 antagonist with an IC50 value of 13 nM against hCCR5. Ancriviroc specifically binds to hCCR5, blocks ligand-induced signal transduction, calcium influx, GTPγS binding, chemotaxis, ligand binding, and HIV-1 entry, induces conformational changes in CCR5, and inhibits infection and replication of R5-tropic HIV-1. | |||||||||||||||||||||
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References
- [1]. Strizki JM, et al. SCH-C (SCH 351125), an orally bioavailable, small molecule antagonist of the chemokine receptor CCR5, is a potent inhibitor of HIV-1 infection in vitro and in vivo. Proc Natl Acad Sci U S A. 2001;98(22):12718-12723. [Content Brief]
- [2]. Saita Y, et al. Transgenic mouse expressing human CCR5 as a model for in vivo assessments of human selective CCR5 antagonists. Eur J Pharmacol. 2005;518(2-3):227-233. [Content Brief]
