GRGDSP
目录号 : GC33323GRGDSP是一种合成的线性RGD肽,是一种整联蛋白(integrin)抑制剂。
Cas No.:91037-75-1
Sample solution is provided at 25 µL, 10mM.
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GRGDSP, a synthetic linear RGD peptide, is an integrin inhibitor.
It is demonstrated that transarterial infusion of GRGDSP (Gly-Arg-Gly-Asp-Ser-Pro integrin-inhibitor which includes RGD-peptide). As a synthetic linear RGD peptide, GRGDSP (Gly-Arg-Gly-Asp-Ser-Pro) can inhibit the adherence of tumor cells to endothelial cells of blood vessels and limit its metastasis[1]. GRGDSP (Gly-Arg-Gly-Asp-Ser-Pro) is used as a soluble integrin-blocking RGD-based peptide. GRGDSP is used widely together with other RGD peptides in integrin research. GRGDSP can be used to modify the surface of cardiovascular implants such as vascular grafts to promote endothelialization[2].
[1]. Qian J, et al. Transarterial administration of integrin inhibitor loaded nanoparticles combined with transarterial chemoembolization for treating hepatocellular carcinoma in a rat model. World J Gastroenterol. 2016 Jun 7;22(21):5042-9. [2]. Patel S, et al. Regulation of endothelial cell function by GRGDSP peptide grafted on interpenetrating polymers. J Biomed Mater Res A. 2007 Nov;83(2):423-33.
Cas No. | 91037-75-1 | SDF | |
Canonical SMILES | Gly-Arg-Gly-Asp-Ser-Pro | ||
分子式 | C22H37N9O10 | 分子量 | 587.58 |
溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg | |
1 mM | 1.7019 mL | 8.5095 mL | 17.019 mL |
5 mM | 0.3404 mL | 1.7019 mL | 3.4038 mL |
10 mM | 0.1702 mL | 0.8509 mL | 1.7019 mL |
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2.
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Regulation of endothelial cell function by GRGDSP peptide grafted on interpenetrating polymers
J Biomed Mater Res A 2007 Nov;83(2):423-33.PMID:17455217DOI:10.1002/jbm.a.31320.
Vascular endothelium plays an important role in preventing thrombogenesis. Bioactive molecules such as fibronectin-derived peptide Gly-Arg-Gly-Asp-Ser-Pro (GRGDSP) can be used to modify the surface of cardiovascular implants such as vascular grafts to promote endothelialization. Here we conjugated GRGDSP peptide to the nonfouling surface of an interpenetrating polymer network (IPN), and investigated the effects of the immobilized GRGDSP molecules on EC functions under static and flow conditions at well-defined GRGDSP surface densities (approximately 0 to 3 pmol/cm2). EC adhesion and spreading increased with GRGDSP surface density, reached a plateau at 1.5 pmol/cm2, and increased further beyond 2.8 pmol/cm2. Cell adhesion and spreading on GRGDSP induced two waves of extracellular signal-regulated kinase (ERK) activation, and 0.2 pmol/cm2 density of GRGDSP was sufficient to activate ERK. EC proliferation rate was not sensitive to GRGDSP surface density, suggesting that cell spreading at low-density of GRGDSP is sufficient to maintain EC proliferation. EC migration on lower-density GRGDSP-IPN surfaces was faster under static condition. With the increase of GRGDSP density, the speed and persistence of EC migration dropped quickly (0.2-0.8 pmol/cm2) and reached a plateau, followed by a slower and gradual decrease (1.5-3.0 pmol/cm2). These data suggest that the changes of EC functions were more sensitive to the increase of GRGDSP density at lower range. Under flow condition with shear stress at 12 dyn/cm2, EC migration was inhibited on GRGDSP-IPN surfaces, which may be attributed to the assembly of large focal adhesions induced by shear stress, suggesting a catch-bond characteristic for RGD-integrin binding. This study provides a rational base for surface engineering of cardiovascular implants.
GRGDSP peptide-bound silicone membranes withstand mechanical flexing in vitro and display enhanced fibroblast adhesion
Biomaterials 2002 Aug;23(15):3159-68.PMID:12102187DOI:10.1016/s0142-9612(02)00062-5.
Mechanobiological studies of cardiac tissue require devices that allow forces to be exerted on cells in vitro. Silicone elastomer is often used in these devices because it is flexible and transparent, permitting optical imaging of the cells. However, native untreated silicone is hydrophobic and is unsuitable for cell culture. Peptides covalently bound to silicone surfaces are examined here for the enhancement of cellular adhesion during in vitro dynamic flexing. A procedure is described for the chemical modification of medical grade silicone membranes with covalently bound GRGDSP peptides. The conditions for mechanical studies of cardiac cell cultures are then duplicated and it is demonstrated that the peptide layers survive 48 h of mechanical flexing in vitro. Specifically, mechanical flexing in vitro of the 30 pmol/cm2 peptide-modified silicone membranes has no significant effect on the amount of peptides that remains bound to the surface. Cardiac fibroblasts display enhanced adhesion to these peptide-bound silicone membranes for at least 24 h of growth, compared with native silicone or tissue culture polystyrene. The effects of serum versus serum-free media on fibroblast growth are also examined.
Neuronal production from induced pluripotent stem cells in self-assembled collagen-hyaluronic acid-alginate microgel scaffolds with grafted GRGDSP/Ln5-P4
Mater Sci Eng C Mater Biol Appl 2017 Jul 1;76:760-774.PMID:28482588DOI:10.1016/j.msec.2017.03.133.
Self-assembled microgel functionalized with peptides was developed and applied to regenerate neurons from induced pluripotent stem cells (iPSCs). Collagen (COL), hyaluronic acid (HA), and alginate (ALG) were modified with methacrylic anhydride (MA), photocrosslinked for patterned particles, grafted with GRGDSP and Ln5-P4, and self-assembled to integrate the microgel into three-dimensional scaffolds. Physicochemical assessments revealed that the ternary microgel scaffolds had an optimal chemical composition at COLMA:HAMA:ALGMA=1:2:1. In fabricating cell-laden constructs, modified GRGDSP/Ln5-P4 in linear self-assembled scaffolds could significantly improve the entrapment efficiency and viability of iPSCs. In addition, GRGDSP/Ln5-P4 in the microgel constructs triggered the differentiation of iPSCs toward neurons, since the percentage of neurite-like cells could be higher than 98% after induction of nerve growth factor. Self-assembled microgel comprising COLMA, HAMA, ALGMA, and GRGDSP/Ln5-P4 may be promising in producing mature neural lineage from iPSCs, to provide better treatment for damaged nervous tissue.
Surface-attached PDMAA-GRGDSP hybrid polymer monolayers that promote the adhesion of living cells
Biomacromolecules 2008 Feb;9(2):543-52.PMID:18179173DOI:10.1021/bm7010714.
Peptide-polymer hybrid molecules are being introduced, where one part of the molecule (i.e., the peptide) promotes the adhesion of living cells, whereas the other part of the molecule (i.e., the synthetic polymer) is known to prevent cell adhesion. The hybrid copolymer, poly(dimethylacrylamide) (PDMAA)-glycine-arginine-glycine-aspartic acid-serine-proline (GRGDSP) was synthesized by first preparing an initiator-modified peptide and in a second step growing the PDMAA block directly off the peptide through atom transfer radical polymerization (ATRP). The PDMAA block length can be varied by adjusting appropriate polymerization conditions, thereby changing progressively the amount of the cell-repelling part of the molecule. The hybrid copolymer was further used to prepare surface-attached peptide-polymer monolayers at planar solid glass substrates through a photochemical immobilization process. By blending of the hybrid copolymer with PDMAA homopolymer (i.e., without peptide), the apparent peptide film concentration can be varied in a very simple manner. The adhesion of human skin fibroblast cells in serum-free medium was investigated as a function of the amount of peptide-polymer in the solution used for film preparation. Cells do not adhere to a pure PDMAA monolayer; however, already 0.02 wt % of peptide in the film is enough to induce cell adhesion, and 0.1 wt % promotes stress-fiber formation within adherent cells. Using lithographical means, chemically micropatterned peptide-polymer films were prepared that allow for a spatial control of the adhesion of living cells and thus they constitute a simple platform for the design of live-cell biochips.
A fibrin or collagen gel assay for tissue cell chemotaxis: assessment of fibroblast chemotaxis to GRGDSP
Exp Cell Res 1999 Mar 15;247(2):543-53.PMID:10066382DOI:10.1006/excr.1998.4364.
Fibroblast chemotaxis is implicated in many physiological processes, including wound healing and morphogenesis. We present a novel assay for chemotaxis of fibroblasts (and other slow-moving tissue cells) in a direct-viewing chamber containing a physiologically relevant three-dimensional fibrin or collagen gel in which long-lasting, spatially continuous gradients have been sustained for at least 24 h, long enough for significant fibroblast migration. This combination of features is not available in any alternative assay of comparable setup simplicity. Using a putative fibroblast chemotactic factor, the fibronectin peptide GRGDSP, we measured human foreskin fibroblast alignment in the direction along the gradient, which followed a biphasic dependence on GRGDSP concentration with an optimal concentration of about 10 nM. Time-lapse video microscopy revealed that cell migration was up the soluble GRGDSP gradient, confirming positive chemotaxis to GRGDSP and rejecting the possibility of dominant haptotaxis down the soluble GRGDSP gradient, that is, up a putative gradient of integrin-mediated adhesion induced by the soluble GRGDSP gradient.