| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
Cell lines | B16-F10 cells and HUVEC |
Preparation Method | Dil-loaded micellar formulations with different Cyclo(RGDyK) densities (0%, 10%, 20%) were incubated with B16-F10 cells or HUVEC in six-well plates for 3 h at 37°C at a final concentration of 0.5 ug/mL or 0.1 ug/mL Dil diluted in culture media, respectively. And the cells incubated with medium were used as negative controls. For the competition experiments, free Cyclo(RGDyK) (0.8 mM for B16-F10 and 1.6 µM for HUVEC) was pre-incubated with cells for 1 h, followed by continued co-incubation with Cyclo(RGDyK)-Dil-PM with 20% cRGDyK for 3 h. Then, cells were washed, trypsinized, and neutralized. After centrifugation at 1200 rpm for 5 min, cells were resuspended in PBS, followed by filtra |
Reaction Conditions | 0.8 mM for B16-F10 and 1.6 µM for HUVEC Cyclo(RGDyK) for 1 h |
Applications | PEG-b-PLGA micelles without or with Cyclo(RGDyK) conjugation loaded with paclitaxel (PTX) or DiI were prepared and characterized. Drug-loaded micelles were stable in solution, with small diameters (<80 nm) and a low critical micelle concentration. |
Animal models | C57BL/6 mice |
Preparation Method | Forty 3-month old female C57BL/6 mic were randomly allocated into four groups: (1) Sham-operated (Sham); (2) ovariectomized; (3) Ovx plus 8-week downhill running exercise (Ex); (4) Ovx plus exercise and received twice weekly injection of Cyclo(RGDyK) protein (a putative anti-irisin receptor agents) (ExRg). |
Dosage form | 2.5 mg/kg Cyclo(RGDyK) twice a week(tail vein injection) |
Applications | Cyclo(RGDyK) administration weakened the exercise-related improvement of vBMD, BV/TV, and ALP intensity in bone. |
| 文献引用 | |
| 产品描述 | Cyclo(RGDyK) is a potent and selective αVβ3 integrin inhibitor with IC50 of 20 nM[1]. PEG-b-PLGA micelles without or with Cyclo(RGDyK) conjugation loaded with paclitaxel (PTX) or DiI were prepared and characterized. Drug-loaded micelles were stable in solution, with small diameters ([5]. A novel drug delivery system Cyclo(RGDyK) -modified Fe3O4 nanoparticles with high DOX load (R-DMP), which combines magnetic targeting, integrin alpha(v)beta3 targeting and high drug loading properties, was developed by chemical coupling both doxorubicin and peptide Cyclo(RGDyK)) on the synthetic dual function magnetic nanoparticles (DMP) using a multi-hand cross-linker poly-L-glutamic acid. D-DMP shows enhanced uptake by integrin alpha(v)beta3 targeting expressing tumor cells and displays stronger cancer cell cytotoxicity[2]. Cyclo(RGDyK) administration weakened the exercise-related improvement of vBMD, BV/TV, and ALP intensity in bone[4]. By blocking irisin receptor (αV/β5), Cyclo(RGDyK) could reduce irisin-induced signalings. When irisin pathways were blocked, some osteoblastogenic genes were decreased, which might contribute to the Cyclo(RGDyK) -induced reduction of osteogenic differentiation[3]. References: |
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