Peptide R
Based on 1 Customer Validation
Peptide R is a cyclic peptide and a specific CXCR4 antagonist. Peptide R exhibits excellent ability to effectively remodel tumor stroma. Peptide R has potential for use in tumor research.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1318232-11-9
- 分子式: C39H57N13O8S2
- 分子量:900.08
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保管条件:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
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CXCR4 |
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Cell Line
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Type | Value | Description | References |
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| HT-29 | IC50 |
5.2 μM
Compound: 2
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Inhibition of 12G5 anti-CXCR4 antibody binding to CXCR4 in human HT29 cells preincubated for 30 mins followed by antibody addition by FACS Canto II cytofluorometric analysis
Inhibition of 12G5 anti-CXCR4 antibody binding to CXCR4 in human HT29 cells preincubated for 30 mins followed by antibody addition by FACS Canto II cytofluorometric analysis
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[PMID: 27571038] |
Peptide R (10 μM; 48-72 h) stably reduces CXCR4 membrane and total CXCR4 protein expression in human glioblastoma U87MG cells over 48 to 72 h of treatment[2].
Peptide R (10 μM; 72 h) reduces proliferation of human glioblastoma U87MG cells by 35% relative to CXCL12-stimulated cells after 72 h of treatment[2].
Peptide R (10 μM; 72 h) significantly reduces the metabolic viability of human glioblastoma U87MG cells after 72 h of treatment[2].
Peptide R (10 μM; 20 h) significantly reduces CXCL12-induced migration of human glioblastoma U87MG cells in a 20 h Transwell assay[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human glioblastoma U87MG cells
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Concentration:10 μM
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Incubation Time:72 h
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Result:Reduced cell number by 35% compared to CXCL12-stimulated cells at 72 h.
Reduced cell number by 20% compared to unstimulated cells at 72 h.
Showed no significant effects at 24 or 48 h.
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Cell Line:human glioblastoma U87MG cells
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Concentration:10 μM
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Incubation Time:72 h
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Result:Caused a significant reduction in metabolic activity of U87MG cells at 72 h.
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Cell Line:human glioblastoma U87MG cells
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Concentration:10 μM
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Incubation Time:20 h
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Result:Significantly reduced the percentage of area occupied by migrating U87MG cells.
Hampered cell migration through membrane pores, with very few cells visible on the lower side of the filter compared to CXCL12-stimulated cells.
Peptide R (2 mg/kg; i.p.; twice per day; 23 days) reduces tumor cellularity and abrogates distant glioblastoma cell dissemination, promotes M1 polarization of GAMs, and impairs intra-tumor vasculature in orthotopic U87MG xenografts in CD1 nude mice[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CD1 nude mice (6-week-old)[2]
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Dosage:2 mg/kg
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Administration:i.p.; twice per day; 23 days (starting on cell implantation day)
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Result:Reduced tumor cellularity via decreased vimentin expression.
Abrogated dissemination of glioblastoma cells to distant cerebral sites, with no vimentin-positive cells detected in the contralateral hemisphere.
Decreased accumulation of CD11b+ and CD68+ glioma-associated microglia/macrophages (GAMs) at the tumor edge, with mean CD11b fluorescence reduced by ~55% and mean CD68 fluorescence reduced by ~50% compared to vehicle-treated mice.
Promoted M1 pro-inflammatory features in GAMs, with a significant increase in mean inducible nitric oxide synthase (iNOS) fluorescence in the tumor core compared to vehicle-treated mice, and a 2-fold increase in the percentage of CD11b-iNOS colocalized area.
Induced stronger astrogliosis (glial fibrillary acidic protein expression) in tumor tissue.
化学情報
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CAS 番号 1318232-11-9
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性状 Solid
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分子量 900.08
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分子式 C39H57N13O8S2
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Color White to off-white
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配列
Arg-Ala-Cys-Arg-Phe-Phe-Cys (disulfide bridge:Cys3-Cys7)
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シーケンスの短縮
RACRFFC (disulfide bridge:Cys3-Cys7)
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
純度とドキュメンテーション
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データシート (267 KB)
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- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Le Joncour V, et al. Seek & Destroy, use of targeting peptides for cancer detection and drug delivery. Bioorg Med Chem. 2018;26(10):2797-2806. [Content Brief]
[2]. Mercurio L, et al. Targeting CXCR4 by a selective peptide antagonist modulates tumor microenvironment and microglia reactivity in a human glioblastoma model. J Exp Clin Cancer Res. 2016;35:55. Published 2016 Mar 25. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Peptide R 関連分類
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