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Product Details

Maraviroc | CCR5 Antagonist

Maraviroc (376348-65-1) is a potent and selective CCR5 antagonist with potent anti-HIV activity. It prevents HIV-1 gp120 binding to CCR5 preventing cell-cell fusion. Maraviroc inhibited MIP-1a (IC50 = 3.3 nM), MIP-1b (IC50 = 7.2 nM), and RANTES (IC50 = 5.2 nM) binding to CCR5-expressing HEK-293.1 Clinically useful antiretroviral drug. Many cancer cells express CCR5: Maraviroc blocked metastasis of basal breast2 and pancreatic cancer3 cells, induced cytotoxic and apoptotic effects in colorectal cancer cells4, reduced metastatic tumor growth in lungs5, and suppresses growth in acute ALL cells6. CCR5 inhibition with maraviroc induced macrophage repolarization with anti-tumoral effects.7

References/Citations

1) Dorr et al. (2005), 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; Antimicrob.Agents Chemother. 49 4721
2) Velasco-Velazquez et al. (2012), CCR5 antagonist blocks metastasis of basal breast cancer cells; Cancer Res. 72 3839
3) Singh et al. (2018), CCR5/CCL5 axis interaction promotes migratory and invasiveness of pancreatic cancer cells; Sci.Rep. 1323
4) Pervaiz et al. (2015), CCR5 blockage by maraviroc induces cytotoxic and apoptotic effects in colorectal cancer cells; Med.Oncol. 32 158
5) Halvorsen et al. (2016), Maraviroc decreases CCL8-mediated migration of CCR5(+) regulatory T cells and reduces metastatic tumor growth in the lungs; Oncoimmunology e1150398
6) Zi et al. (2017), Treatment with the C-C chemokine receptor type 5(CCR5)-inhibitor maraviroc suppresses growth and induces apoptosis of acute lymphoblastic leukemia cells; Am.J.Cancer Res. 869
7) Halama et al. (2016), Tumoral Immune Cell Exploitation in Colorectal Cancer Metastases Can Be targeted Effectively by Anti-CCR5 Therapy in Cancer Patients; Cancer Cell 29 587

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Catalog#  10-4260-0005

$59.00
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Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee.
 
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CAS:
376348-65-1
Catalog Number:
10-4260
Activity:
CCR5 Antagonist
Chemical Name:
4,4-difluoro-N-[(1S)-3-[(1R,5S)-3-(3-methyl-5-propan-2-yl-1,2,4-triazol-4-yl)-8-azabicyclo[3.2.1]octan-8-yl]-1-phenylpropyl]cyclohexane-1-carboxamide
Molecular Weight:
513.68
Molecular Formula:
C29H41F2N5O
Solubility:
Soluble in DMSO (>25 mg/ml)
Physical Properties:
White solid
Purity:
>98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C (des.)
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT
Alternate Name:
UK-427,857
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

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