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Cyclo(RGDyK) Trifluoroacetate

* Please kindly note that our products are not to be used for therapeutic purposes and cannot be sold to patients.

Cyclo(RGDyK) is a potent and selective αVβ3 integrin inhibitor with IC50 of 20 nM.

Category

Peptide Inhibitors

Catalog number

BAT-010216

CAS number

250612-42-1

Molecular Formula

C31H43F6N9O12

Molecular Weight

847.71

Size	Price	Stock	Quantity
100 mg	$519	In stock

Specification
Reference Reading

IUPAC Name

2-[(2S,5R,8S,11S)-8-(4-aminobutyl)-11-[3-(diaminomethylideneamino)propyl]-5-[(4-hydroxyphenyl)methyl]-3,6,9,12,15-pentaoxo-1,4,7,10,13-pentazacyclopentadec-2-yl]acetic acid; 2,2,2-trifluoroacetic acid

Synonyms

Cyclo (RGDyK); Cyclo RGDyK; Cyclo(RGDyK) trifluoroacetate

Appearance

Solid Powder

Purity

>98%

Sequence

cyclo[Arg-Gly-Asp-D-Tyr-Lys].2TFA

Storage

Store at -20°C

Solubility

Soluble in DMSO (100mg/mL), Water (100mg/mL), Ethanol (20mg/mL)

InChI

InChI=1S/C27H41N9O8.2C2HF3O2/c28-10-2-1-4-18-24(42)34-17(5-3-11-31-27(29)30)23(41)32-14-21(38)33-20(13-22(39)40)26(44)36-19(25(43)35-18)12-15-6-8-16(37)9-7-15;2*3-2(4,5)1(6)7/h6-9,17-20,37H,1-5,10-14,28H2,(H,32,41)(H,33,38)(H,34,42)(H,35,43)(H,36,44)(H,39,40)(H4,29,30,31);2*(H,6,7)/t17-,18-,19+,20-;;/m0../s1

InChI Key

CDDUWKKOPQABPG-TVSMIREGSA-N

Canonical SMILES

C1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CCCN=C(N)N)CCCCN)CC2=CC=C(C=C2)O)CC(=O)O.C(=O)(C(F)(F)F)O.C(=O)(C(F)(F)F)O

1.Development of long-circulating zwitterionic cross-linked micelles for active-targeted drug delivery.

Lin W, Ma G, Kampf N, Yuan ZF, Chen S. Biomacromolecules. 2016 Apr 6. [Epub ahead of print]

Blood stability, active targeting and controlled drug release are the most important features to design desirable drug carriers. Here, we demonstrate a zwitterionic biodegradable cross-linked micelle based on a block copolymer, which utilizes poly(carboxybetaine methacrylate) (PCBMA) as hydrophilic segment, poly(ε-caprolactone) (PCL) as biodegradable hydrophobic segment, poly(S-2-hydroxyethyl-O-ethyl dithiocarbonate methacrylate) (PSODMA) block as thiol protecting segment for cross-linking, and cyclic Arg-Gly-Asp-d-Tyr-Lys [c(RGDyK)] as targeting ligand. As a result, this micelle possessed excellent colloidal stability at high dilution and in 50% fetal bovine serum (FBS). In vitro drug release experiment showed no burst release under physiological conditions but accelerated drug release in mimicking tumor tissue environment. In vivo tests showed that the drug-loaded micelles had prolonged half-life in bloodstream, enhanced therapeutic efficiency, reduced cardiac toxicity and bio-toxicity compared with free drug formulation.