| Identification | Back Directory | [Name]
Cyclic Arg-Gly-Asp-D-Tyr-Lys | [CAS]
250612-42-1 | [Synonyms]
Cyclic Arg-Gly-Asp-D-Tyr-Lys
Cyclo(RGDyK) trifluoroacetate
CCyclic Arg-Gly-Asp-D-Tyr-Lys
Cyclo(L-arginylglycyl-L-α-aspartyl-D-tyrosyl-L-lysyl) di2,2,2-Trifluoroacetic acid salt | [Molecular Formula]
C29H42F3N9O10 | [MDL Number]
MFCD20134101 | [MOL File]
250612-42-1.mol | [Molecular Weight]
733.7 |
| Chemical Properties | Back Directory | [storage temp. ]
Inert atmosphere,2-8°C | [solubility ]
Soluble in DMSO | [form ]
Solid | [color ]
White to off-white | [Sequence]
cyclo(Arg-Gly-Asp-{d-Tyr}-Lys) | [InChIKey]
KTQFOJMRRQLTAN-CNDMKARKNA-N | [SMILES]
C(F)(F)(F)C(=O)O.C(C1C=CC(O)=CC=1)[C@H]1NC([C@@H](NC(CNC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCCN)NC1=O)=O)CC(=O)O)=O |&1:15,18,25,36,r| |
| Hazard Information | Back Directory | [Uses]
Cyclo(RGDyK) trifluoroacetate is a potent and selective αVβ3 integrin inhibitor with an IC50 of 20 nM. | [Biological Activity]
Cyclo(RGDyK) is a potent and selective αVβ3 integrin inhibitor with IC50 of 20 nM. | [in vitro]
Cyclo(RGDyK) showed higher affinity and selectivity for αVβ3 than αVβ5 and αIIbβ3. Cyclo(RGDyK)-bound micelles (TPM) promoted cell-specific uptake of DiI by B16-F10 cells and HUVECs through integrin-mediated endocytosis compared to Cyclo(RGDyK)-free micelles (NPM). | [in vivo]
Cyclo(RGDyK) (1 nmol, iv) inhibits the increase in αVβ3 integrin expression in the intima of left stenotic carotid arteries in apoE?/? mice. | [target]
| Target | Value | | αVβ3 integrin | 20 nM |
| [IC 50]
αvβ3: 20 nM (IC50) | [References]
[1] Haubner R, 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 |
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