Maraviroc

Catalog # Availability Size / Price Qty
3756/10
3756/50
Maraviroc | CAS No. 376348-65-1 | Chemokine Receptor Antagonists
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Description: Selective CCR5 antagonist
Alternative Names: UK-427857

Chemical Name: 4,4-Difluoro-N-{(1S)-3-[3-(3-isopropyl- 5-methyl-4H-1,2,4-triazol-4-yl)- 8-azabicyclo[3.2.1]oct-8-yl]-1- phenylpropyl}cyclohexanecarboxamide

Purity: ≥99%

Product Details
Citations (7)
Supplemental Products
Reviews

Biological Activity

Maraviroc is a selective CCR5 antagonist; displays potent anti-HIV-1 activity. Prevents the interaction of HIV-1 gp120 and CCR5 (IC50 = 6.4 nM), inhibiting HIV-1 entry. Exhibits antinociceptive effects in a rat model of neuropathic pain. Also inhibits CCL3 (MIP-1α) binding to CCR5. Orally bioavailable.

Technical Data

M.Wt:
513.67
Formula:
C29H41F2N5O
Solubility:
Soluble to 75 mM in DMSO and to 100 mM in ethanol
Purity:
≥99%
Storage:
Store at +4°C
CAS No:
376348-65-1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Licensing Caveats:
Sold for research purposes under agreement from Viiv.

Background References

  1. Simultaneous blockade of IL-6 and CCL5 signaling for synergistic inhibition of triple-negative breast cancer growth and metastasis
    K Jin, NB Pandey, AS Popel
    Breast Cancer Res., 2018;20(1):54.
  2. Macrophage migration inhibitory factor-CXCR4 is the dominant chemotactic axis in human mesenchymal stem cell recruitment to tumors.
    Lourenco S, Teixeira V, Kalber T, Jose R, Floto R, Janes S
    J Immunol, 2015;194(7):3463-74.
  3. C/EBP? drives interactions between human MAIT cells and endothelial cells that are important for extravasation
    CH Lee, HH Zhang, SP Singh, L Koo, J Kabat, H Tsang, TP Singh, JM Farber
    Elife, 2018;7(0):.
  4. Breast cancer cells condition lymphatic endothelial cells within pre-metastatic niches to promote metastasis.
    Lee E, Fertig E, Jin K, Sukumar S, Pandey N, Popel A
    Nat Commun, 2014;5(0):4715.
  5. Biased signaling at chemokine receptors.
    Corbisier J, Gales C, Huszagh A, Parmentier M, Springael J
    J Biol Chem, 2015;290(15):9542-54.
  6. Astrocytic orosomucoid-2 modulates microglial activation and neuroinflammation
    M Jo, JH Kim, G Song, M Seo, E Mi Hwang, K Suk
    J. Neurosci, 2017;0(0):.
  7. Maraviroc (UK-427,857), a potent, orally bioavailable, and selective small-molecule inhibitor of chemokine receptor CCR5 with broad-spectrum anti-human immunodeficiency virus type 1 activity.
    Dorr et al.
    Antimicrob.Agents Chemother., 2005;49:4721
  8. New insights into the mechanisms whereby low molecular weight CCR5 ligands inhibit HIV-1 infection.
    Garcia-Perez et al.
    J.Biol.Chem., 2011;286:4978
  9. Maraviroc reduces neuropathic pain through polarization of microglia and astroglia - Evidence from in vivo and in vitro studies.
    Piotrowska et al.
    Neuropharmacology, 2016;S0028-3908:30164
  10. Fresh from the pipeline - mara.
    Kuritzkes et al.
    Nat.Rev.Drug Discov., 2008;7:15

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