Cyclo(RGDyK)

製品コードS7844 バッチS784403

印刷

化学情報

 Chemical Structure Synonyms N/A Storage
(From the date of receipt)
3 years -20°C powder
1 years -80°C in solvent
化学式

C31H43F6N9O12

分子量 847.72 CAS No. 250612-42-1
Solubility (25°C)* 体外 DMSO 100 mg/mL (117.96 mM)
Water 100 mg/mL (117.96 mM)
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液(一定の濃度)を調合する

生物活性

製品説明 Cyclo(RGDyK) is a potent and selective αVβ3 integrin inhibitor with IC50 of 20 nM.
in vitro Cyclo(RGDyK) shows high affinity and selectivity for αVβ3 over αVβ5 and αIIbβ3. [1] Cyclo(RGDyK)-conjugated micelles (TPM) facilitated the cell-specific uptake of DiI into B16-F10 cells and HUVECs via integrin-mediated endocytosis compared with Cyclo(RGDyK) -free micelles (NPM). [2]
in vivo In apoE−/− mice, Cyclo(RGDyK) (1 nmol, i.v.) inhibits the increase of αVβ3 integrin expression in the intima of the left stenotic carotid artery. [2]

プロトコル(参考用のみ)

キナーゼアッセイ Biological Assay
Purification of the proteins as well as the isolated integrin-binding assay are carried. The inhibitory capacities of the cyclic peptides are quantified by measuring their effect on the interactions between immobilized integrin and biotinylated soluble ligands (vitronectin or fibrinogen). Recombinant human αVβ3 and recombinant soluble human αVβ5 produced by similar procedures are used in this study and give identical results to the native placental integrins αVβ3 and αVβ5. The integrin preparations differed somewhat over time; thus the linear peptide Gly-Arg-Gly-Asp-Ser-Pro-Lys as well as the αVβ3-selective cyclo(-Arg-Gly-Asp-D-Phe-Val-) are used as internal standards to allow interassay comparability.
動物実験 動物モデル ApoE−/− mice
投薬量 1 nmol
投与方法 i.v.

カスタマーフィードバック

Data from [Data independently produced by , , Carcinogenesis, 2018, doi:10.1093/carcin/bgy146]

Selleckの高級品が、幾つかの出版された研究調査結果(以下を含む)で使われた:

Regulation of the integrin αVβ3- actin filaments axis in early osteogenic differentiation of human mesenchymal stem cells under cyclic tensile stress [ Cell Commun Signal, 2023, 10.1186/s12964-022-01027-7] PubMed: 37904190
Molecular signaling from microglia impacts macroglia autophagy and neurons survival in glaucoma [ iScience, 2023, 26(6):106839] PubMed: 37250793
Integrin αVβ3 Signaling in the Progression of Osteoarthritis Induced by Excessive Mechanical Stress [ Inflammation, 2023, 46(2):739-751] PubMed: 36480128
Inhibition of Integrin αvβ3-FAK-MAPK signaling constrains the invasion of T-ALL cells [ Cell Adh Migr, 2023, 17(1):1-14] PubMed: 36944577
Inhibition of Integrin αvβ3-FAK-MAPK signaling constrains the invasion of T-ALL cells [ Cell Adhesion & Migration, 2023, 17(1)] PubMed: None
Integrin α2 and β1 Cross-Communication with mTOR/AKT and the CDK-Cyclin Axis in Hepatocellular Carcinoma Cells [ Cancers (Basel), 2022, 14(10)2430] PubMed: 35626034
Renal protection induced by physical exercise may be mediated by the irisin/AMPK axis in diabetic nephropathy [ Sci Rep, 2022, 12(1):9062] PubMed: 35641586
Regulation of the integrin αVβ3- actin filaments axis in early osteogenesis of human fibroblasts under cyclic tensile stress [ Stem Cell Res Ther, 2021, 12(1):523] PubMed: 34620239
M2 polarization of tumor-associated macrophages is dependent on integrin β3 via peroxisome proliferator-activated receptor-γ up-regulation in breast cancer. [ Immunology, 2020, 20] PubMed: 32311768
Spontaneous Extracellular Matrix Accumulation in a Human in vitro Model of Renal Fibrosis Is Mediated by αV Integrins [ Nephron, 2019, 10.1159/000499506] PubMed: 31048591

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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