>>Peptides>>Cyclo(RGDyK)

Cyclo(RGDyK)

Catalog No.GC13923

Cyclo(RGDyK)는 IC50 값이 20 nM인 강력하고 선택적인 αVβ3 인테그린 억제제입니다.

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Cyclo(RGDyK) Chemical Structure

Cas No.: 250612-42-1

Size 가격 재고 수량
10mM (in 1mL DMSO)
US$156.00
재고 있음
5mg
US$102.00
재고 있음
10mg
US$167.00
재고 있음
25mg
US$334.00
재고 있음
50mg
US$547.00
재고 있음
100mg
US$825.00
재고 있음

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Sample solution is provided at 25 µL, 10mM.

Product has been cited by 2 publications

Product Documents

Quality Control & SDS

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Protocol

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:

[1]. 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.
[2]. 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.

Background

Cyclo(RGDyK)는 IC50 값이 20 nM인 강력하고 선택적인 αVβ3 인테그린 억제제입니다. [1]

팔리탁셀(PTX) 또는 DiI로 로드된 Cyclo(RGDyK) 결합 여부가 없는 PEG-b-PLGA 마이셀을 제조하고 특성화했습니다. 약물이 로드된 마이셀은 용액에서 안정적이며 직경이 작습니다 ([5]).

화학적 결합을 통해 독소르빈과 펩타이드 Cyclo(RGDyK)를 합성된 이중 기능 자석 나노입자(DMP)에 부착하여, 자기 타겟팅, 인테그린 알파(v)베타3 타겟팅 및 고용량 약물 전달 기능을 결합한 새로운 약물 전달 시스템인 Cyclo(RGDyK)-수정 Fe3O4 나노입자 (R-DMP)가 개발되었다. D-DMP는 인테그린 알파(v)베타3을 발현하는 종양 세포에서 강화된 흡수를 보이며 더 강한 항암 세포 독성을 나타낸다[2].

Cyclo(RGDyK) 투여는 뼈의 vBMD, BV/TV 및 ALP 강도에 대한 운동 관련 개선을 약화시켰습니다[4]. Irisin 수용체 (αV/β5)를 차단함으로써 Cyclo(RGDyK)는 irisin 유도 신호를 감소시킬 수 있습니다. Irisin 경로가 차단될 때 일부 골모세포 생성 유전자가 감소되어 Cyclo(RGDyK)-유도 골형성 분화의 감소에 기여할 수 있습니다[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.

Chemical Properties

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
Solubility 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.

Complete Stock Solution Preparation Table

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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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리뷰

Review for Cyclo(RGDyK)

Average Rating: 5 ★★★★★ (Based on Reviews and 22 reference(s) in Google Scholar.)

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