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| Targets |
GRGDSPK targets integrins, a family of cell surface receptors that mediate cell-extracellular matrix adhesion. By containing the RGD sequence, it competitively binds to integrins, blocking integrin-fibronectin binding and inhibiting integrin-mediated cell adhesion, migration, and signaling.
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| ln Vitro |
GRGDSPK (EMD 56574; RGD; 0.1-50 μM; for 4 days) inhibits mineralization in parietal bones separated from pregnant Sprague-Dawley rats on day 18 in a dose-dependent manner as determined by calcium content and 70 bone tissue area. 1]. For four days, GRGDSPK (10, 50 μM) can drastically alter the shape of bones and kill osteoblasts and mineralized matrix tissue [1]. When added to the culture medium, GRGDSPK (RGD; 250 μM) greatly increases the average size of wild-type cell aggregates and effectively prevents integrin-fibronectin binding [2]. Wild-type mesendodermal progenitors show significantly decreased adhesion and work upon the addition of GRGDSPK (250 μM), suggesting that the observed detachment parameters are specific for fibronectin and involve integrins expressed in mesendodermal progenitors [2]. Reduced cleavage, which is a dose-dependent effect of GRGDSPK (containing RGD, 1.5 mM, 1.0 mM, and 0.5 mM) and RGD-modified peptides, prevents sperm from fertilizing bovine oocytes [3].
In vitro, GRGDSPK (250 uM) effectively blocks integrin-fibronectin binding and significantly increases the average size of wild-type cell aggregates. At 10-50 uM for 4 days, it dramatically alters bone morphology, disrupting osteoblast and mineralized matrix organization. It dose-dependently inhibits mineralization in rat parietal bone organ cultures. |
| ln Vivo |
In vivo, GRGDSPK is used to study the role of integrins in bone formation and resorption. As a competitive integrin inhibitor, it modulates cell-matrix interactions in vivo. Specific in vivo efficacy data are limited, as the compound is primarily used as a research tool in ex vivo and in vitro assays.
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| Enzyme Assay |
In vitro integrin binding assays for GRGDSPK are performed using purified integrin proteins or cell surface integrins. The compound is incubated with integrin-coated plates or integrin-expressing cells in the presence of labeled fibronectin or other RGD-containing ligands. Binding inhibition is measured by ELISA or fluorescence-based methods. IC50 values are determined from competition curves.
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| Cell Assay |
Cellular assays for GRGDSPK are conducted using various cell types that express integrins, such as fibroblasts, osteoblasts, or mesendodermal progenitors. Cells are treated with GRGDSPK (10-250 uM) for 1-4 days. Cell adhesion is assessed by measuring attached cells after washing. Cell migration is evaluated by scratch or Transwell assays. Integrin signaling is assessed by Western blot for FAK or other downstream effectors.
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| Animal Protocol |
In vivo animal studies for GRGDSPK are conducted in rat models to study bone formation and resorption. Parietal bones from 18-day-old rat embryos are isolated and cultured with GRGDSPK (10-50 uM) for 4 days. Mineralization is assessed by calcium content measurement and histomorphometric analysis of bone area.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of GRGDSPK are not extensively characterized, as it is a research peptide used primarily in in vitro assays. The compound has a molecular weight of 715.76 and formula C28H49N11O11. It is a solid stored at -20degC. As a peptide, it is susceptible to proteolytic degradation and has limited oral bioavailability.
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| Toxicity/Toxicokinetics |
Toxicological data for GRGDSPK are limited. As a peptide that inhibits integrin-mediated adhesion, it is generally considered non-toxic at concentrations used in research (10-250 uM). Standard laboratory safety precautions apply. The compound is for research use only.
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| References |
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| Additional Infomation |
GRGDSPK (EMD 56574) is a research-use peptide not approved for clinical therapeutic applications. It is widely used as a tool to study integrin function, cell adhesion, migration, and signaling. It is also used to study the role of integrins in bone formation and resorption. The compound is for research use only and not for human therapeutic application.
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| Molecular Formula |
C28H49N11O11
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| Molecular Weight |
715.75576
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| Exact Mass |
715.361
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| CAS # |
111119-28-9
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| Related CAS # |
GRGDSPK TFA
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| PubChem CID |
130667
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| Appearance |
White to off-white solid powder
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| Density |
1.59 g/cm3
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| Index of Refraction |
1.672
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| LogP |
-10.7
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| Hydrogen Bond Donor Count |
12
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| Hydrogen Bond Acceptor Count |
14
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| Rotatable Bond Count |
23
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| Heavy Atom Count |
50
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| Complexity |
1250
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| Defined Atom Stereocenter Count |
5
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| SMILES |
C1C[C@H](N(C1)C(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)CNC(=O)[C@H](CCCN=C(N)N)NC(=O)CN)C(=O)N[C@@H](CCCCN)C(=O)O
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| InChi Key |
ZRVZOBGMZWVJOS-VMXHOPILSA-N
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| InChi Code |
InChI=1S/C28H49N11O11/c29-8-2-1-5-16(27(49)50)37-25(47)19-7-4-10-39(19)26(48)18(14-40)38-24(46)17(11-22(43)44)36-21(42)13-34-23(45)15(35-20(41)12-30)6-3-9-33-28(31)32/h15-19,40H,1-14,29-30H2,(H,34,45)(H,35,41)(H,36,42)(H,37,47)(H,38,46)(H,43,44)(H,49,50)(H4,31,32,33)/t15-,16-,17-,18-,19-/m0/s1
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| Chemical Name |
(2S)-6-amino-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[(2-aminoacetyl)amino]-5-(diaminomethylideneamino)pentanoyl]amino]acetyl]amino]-3-carboxypropanoyl]amino]-3-hydroxypropanoyl]pyrrolidine-2-carbonyl]amino]hexanoic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.3971 mL | 6.9856 mL | 13.9712 mL | |
| 5 mM | 0.2794 mL | 1.3971 mL | 2.7942 mL | |
| 10 mM | 0.1397 mL | 0.6986 mL | 1.3971 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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