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Submit ReviewMaraviroc 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.
Sold for research purposes under agreement from Viiv.
Maraviroc is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Antiviral Library and Tocriscreen FDA-Approved Drugs. 了解 Tocris 化合物库的更多信息。
分子量 | 513.67 |
公式 | C29H41F2N5O |
储存 | Store at +4°C |
纯度 | ≥99% (HPLC) |
CAS Number | 376348-65-1 |
PubChem ID | 483407 |
InChI Key | GSNHKUDZZFZSJB-ILVMPNSOSA-N |
Smiles | O=C(C4CCC(F)(F)CC4)N[C@@H](CCN2C3CCC2CC(N5C(C)=NN=C5C(C)C)C3)C1=CC=CC=C1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 38.53 | 75 | |
ethanol | 51.37 | 100 |
以下数据基于产品分子量 513.67。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.95 mL | 9.73 mL | 19.47 mL |
5 mM | 0.39 mL | 1.95 mL | 3.89 mL |
10 mM | 0.19 mL | 0.97 mL | 1.95 mL |
50 mM | 0.04 mL | 0.19 mL | 0.39 mL |
参考文献是支持产品生物活性的出版物。
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 PMID: 16251317
Garcia-Perez et al (2011) New insights into the mechanisms whereby low molecular weight CCR5 ligands inhibit HIV-1 infection. J.Biol.Chem. 286 4978 PMID: 21118814
Kuritzkes et al (2008) Fresh from the pipeline - mara. Nat.Rev.Drug Discov. 7 15
Piotrowska et al (2016) Maraviroc reduces neuropathic pain through polarization of microglia and astroglia - Evidence from in vivo and in vitro studies. Neuropharmacology S0028-3908 30164 PMID: 27117708
If you know of a relevant reference for Maraviroc, please let us know.
关键词: Maraviroc, Maraviroc supplier, UK-427857, HIV-1, gp120, CCR5, chemokine, receptors, ligands, selective, antagonists, HIV, Rantes, Chemokine, CC, Receptors, 3756, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 Maraviroc 的部分引用包括:
Hundeyin et al (2019) Innate αβ T cells Mediate Antitumor Immunity by Orchestrating Immunogenic Macrophage Programming. Cancer Discov PMID: 31266770
Lourenco et al (2015) Macrophage migration inhibitory factor-CXCR4 is the dominant chemotactic axis in human mesenchymal stem cell recruitment to tumors. J Immunol 194 3463 PMID: 25712213
Kim (2018) Hepatic stellate cells secrete Ccl5 to induce hepatocyte steatosis. Sci Rep 8 7499 PMID: 29760499
Lin et al (2017) Lactate-activated macrophages induced aerobic glycolysis and epithelial-mesenchymal transition in breast cancer by regulation of CCL5-CCR5 axis: a positive metabolic feedback loop. Oncotarget 8 110426 PMID: 29299159
Piotrowska et al (2016) Maraviroc reduces neuropathic pain through polarization of microglia and astroglia - Evidence from in vivo and in vitro studies. Neuropharmacology S0028-3908 30164 PMID: 27117708
Marciniak et al (2015) The Chemokine MIP-1α/CCL3 impairs mouse hippocampal synaptic transmission, plasticity and memory. Sci Signal 5 15862 PMID: 26511387
Kuratli et al (2018) Water Filtered Infrared A and Visible Light (wIRA/VIS) Irradiation Reduces Chlamydia trachomatis Infectivity Independent of Targeted Cytokine Inhibition. Front Microbiol 9 2757 PMID: 30524392
您是否知道使用了 Tocris Maraviroc 的优秀论文? 请告知我们.
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Receptor antagonists (SB225002: for CXCR2, AMD3465: for CXCR4, RS504393: for CCR2 and Maraviroc: for CCR5) at 10 μM
We ordered this product, combining with another inhibitor, to confirm the migration.To confirm that tested product induces migration, we also screen all MAPK inhibitors and MIF receptor antagonists
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意,Tocris 仅会向正规科研企业/机构地址发送文献。
Rheumatoid arthritis (RA) is a chronic destructive inflammatory autoimmune disease that results from a breakdown in immune tolerance, for reasons that are as yet unknown. This poster summarizes the pathology of RA and the inflammatory processes involved, as well as describing some of the epigenetic modifications associated with the disease and the potential for targeting these changes in the discovery of new treatments.