Cyclo(RGDyK) trifluoroacetate |
| رقم الكتالوجGC13923 |
سيكلو (RGDyK) هو مثبط قوي وانتقائي لمستقبل αVβ3 الذي يعمل بتركيز تثبيط 20 نانومتر.
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Cas No.: 250612-42-1
Sample solution is provided at 25 µL, 10mM.
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:
[1]: Haubner R, Wester HJ, et,al. Glycosylated RGD-containing peptides: tracer for tumor targeting and angiogenesis imaging with improved biokinetics. J Nucl Med. 2001 Feb;42(2):326-36. PMID: 11216533.
[2]: Guo L, Ding W, et,al. The C(RgdyK)-conjugated Fe3O4 nanoparticles with high drug load for dual-targeting integrin alpha(v)beta3-expressing cancer cells. J Nanosci Nanotechnol. 2014 Jul;14(7):4858-64. doi: 10.1166/jnn.2014.8691. PMID: 24757954.
[3]: Kim H, Wrann CD, et,al. Irisin Mediates Effects on Bone and Fat via αV Integrin Receptors. Cell. 2018 Dec 13;175(7):1756-1768.e17. doi: 10.1016/j.cell.2018.10.025. Erratum in: Cell. 2019 Jul 11;178(2):507-508. PMID: 30550785; PMCID: PMC6298040.
[4]:Zhao R, Zhou Y, et,al. Irisin Regulating Skeletal Response to Endurance Exercise in Ovariectomized Mice by Promoting Akt/β-Catenin Pathway. Front Physiol. 2021 Mar 25;12:639066. doi: 10.3389/fphys.2021.639066. PMID: 33841178; PMCID: PMC8027323.
[5]:Yin J, Li Z, et,al. Cyclic RGDyK conjugation facilitates intracellular drug delivery of polymeric micelles to integrin-overexpressing tumor cells and neovasculature. J Drug Target. 2011 Jan;19(1):25-36. doi: 10.3109/10611861003663531. Epub 2010 Mar 16. PMID: 20233083.
| Cell experiment [1]: | |
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 ( |
| Animal experiment [2]: | |
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. |
References: | |
| Cas No. | 250612-42-1 | SDF | |
| Chemical Name | 2,2,2-trifluoroacetic acid compound with 2-((1Z,2S,3Z,5R,6Z,8S,9Z,11S,12Z)-8-(4-aminobutyl)-11-(3-guanidinopropyl)-3,6,9,12,15-pentahydroxy-5-(4-hydroxybenzyl)-1,4,7,10,13-pentaazacyclopentadeca-3,6,9,12,15-pentaen-2-yl)acetic acid (2:1) | ||
| Canonical SMILES | NCCCC[C@@]1([H])/C(O)=N/[C@@](/C(O)=N/C/C(O)=N/[C@@](/C(O)=N/[C@](/C(O)=N/1)([H])CC2=CC=C(O)C=C2)([H])CC(O)=O)([H])CCCNC(N)=N.FC(F)(F)C(O)=O.FC(F)(F)C(O)=O | ||
| Formula | C31H43F6N9O12 | M.Wt | 847.72 |
| الذوبان | DMSO : 100mg/mL; Water : 100mg/mL | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.1796 mL | 5.8982 mL | 11.7963 mL |
| 5 mM | 0.2359 mL | 1.1796 mL | 2.3593 mL |
| 10 mM | 0.118 mL | 0.5898 mL | 1.1796 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.50%
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Average Rating: 5 (Based on Reviews and 22 reference(s) in Google Scholar.)
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