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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- No. CAS: 370893-06-4
- Fòrmula: C28H37BrN4O3
- Peso molecular:557.52
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Almacenamiento:
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Actividad biológica
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Chemical Information
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Actividad biológica
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HIV-1 |
CCR5 13 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| U-87MG ATCC | IC50 |
0.6 nM
Compound: 1
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Concentration required to inhibit the entry of HIV-1 reporter virus (ADA) into U-87 cells by 50%
Concentration required to inhibit the entry of HIV-1 reporter virus (ADA) into U-87 cells by 50%
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[PMID: 12086500] |
Ancriviroc (0.3-10 nM; 1 h) potently inhibits the binding of RANTES to CCR5 expressed on the membrane of CHO cells, with a Ki value of 2.9 nM[1].
Unlabeled Ancriviroc (10 μM, 2 h) binds to CCR5 on B550 cells with high affinity, with a Kd value of 9.27 nM and a Bmax value of 1.98 × 10-4 fmol/cell[1].
Ancriviroc inhibits agonist-induced CCR5 activation in CHO-CCR5 cell membranes, with an IC50 of approximately 16 nM for MIP-1β-induced [35S]GTPγS binding[1].
Ancriviroc (1 h) inhibits the entry of R5 envelope-pseudotyped HIV-1 into U87-CD4-CCR5 cells, with a mean IC50 of 0.69 nM[1].
Ancriviroc (SCH-351125) (at concentrations up to 10000 nM for 3 h) potently inhibits the binding of [125I]-CCL3 to membranes of B300-19 cells expressing human CCR5, with an IC50 of 13 nM; it shows no activity against mouse CCR5 even at concentrations as high as 10000 nM[2].
Ancriviroc (administered 1 min prior to CCL3) inhibits CCL3-induced intracellular Ca2+ elevation in CCR5-expressing B300-19 cells, with an IC50 of 81 nM; it shows no activity against mouse CCR5 even at concentrations as high as 10000 nM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:B550 cells (BayF3 murine pro-B cell line stably expressing human CCR5)
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Concentration:0.01 nM-1 μM
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Incubation Time:1.5 h
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Result:Inhibited MIP-1β-induced chemotaxis of B550 cells with an IC50 of less than 1 nM, and had no chemoattractant activity itself.
Ancriviroc (0.01-10 mg/kg; p.o.; single administration) dose-dependently occupies CCR5 receptors in CCR5 transgenic mice, with an ED50 of 0.10 mg/kg, and achieves nearly complete receptor occupancy at doses of 1 mg/kg and 10 mg/kg[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C.B-17 scid/scid (HIV-1 infection model via implantation of human fetal thymus and liver)[1]
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Dosage:3 mg/kg per day; 10 mg/kg per day; 30 mg/kg per day
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Administration:p.o.; twice daily; 28 days
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Result:Reduced p24 levels and viral RNA significantly relative to untreated mice at 3 mg/kg per day and 10 mg/kg per day.
Achieved undetectable p24 antigen and reduced viral RNA by 3.6 log10 compared with untreated mice at 30 mg/kg per day.
Reduced MHC class I expression on implant cells in a dose-dependent manner compared with untreated mice.
Chemical Information
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No. CAS 370893-06-4
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Peso molecular 557.52
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Fòrmula C28H37BrN4O3
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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
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Synonyms
SCH-351125
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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