| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg | |||
| Other Sizes |
| Targets |
GPRP acetate (0, 2 and 4 mM) stimulates oxidant enzyme production [1].
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|---|---|
| ln Vitro |
GPRP acetate (0, 2 and 4 mM) stimulates oxidant enzyme production [1].
GPRP inhibits ADP-induced platelet aggregation in platelet-rich plasma (PRP).[1] GPRP inhibits fibrinogen polymerization by binding to fibrinogen polymerization sites and modifying glutamine residues in the α- and γ-chains of fibrinogen.[1] In PRP activated via intrinsic pathway, GPRP (2 mM and 4 mM) leads to higher peak levels of free thrombin and larger area under the thrombin generation curve compared to control without GPRP.[1] In the presence of 4 mM GPRP, peak thrombin and area under the curve were 30–40% higher than in absence of GPRP.[1] |
| ln Vivo |
By promoting weight loss and engraftment, GPRP acetate (100 mg/kg; intraperitoneally, once daily for 10 days) dramatically lowers glucose enzyme sodium sulfate (DSS)-induced inflammation [3].
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| Enzyme Assay |
Thrombin generation was measured in platelet-rich plasma (PRP) activated with Actin FSL and CaCl₂.
Aliquots were taken at 15-second intervals and mixed with substrate solution containing S-2238. Reaction was stopped with acetic acid, and absorbance was measured at 405 nm. Thrombin activity was expressed as equivalent amount of thrombin, including α₂-macroglobulin–thrombin complex.[1] |
| Cell Assay |
Platelet-rich plasma (PRP) was prepared from whole blood collected in citrate from healthy volunteers.
PRP platelet count was adjusted to 250,000/µL using autologous platelet-poor plasma. PRP was incubated with or without GPRP for 60 seconds before activation with Actin FSL and CaCl₂.[1] |
| Animal Protocol |
Animal/Disease Models: C57BL/6 mice dextran sodium sulfate (DSS)-induced colitis [3]
Doses: 100 mg/kg Route of Administration: intraperitoneal (ip) injection; 100 mg/kg, one time/day for 10 days Experimental Results: Significant Dramatically inhibited weight loss in colitis mice, diminished DSS-induced mortality and colon length shortening, and diminished tissue damage and inflammatory cell infiltration. Mice with colitis have diminished levels of inflammatory cytokines. |
| References | |
| Additional Infomation |
GPRP is a fibrinogen-related peptide currently in the preclinical research stage as an antithrombotic drug. [1] It inhibits fibrinogen-dependent platelet aggregation and fibrin polymerization. [1] By inhibiting fibrin formation, GPRP reduces the adsorption of free thrombin on fibrin (antithrombin I effect), thereby leading to an increase in the level of free thrombin after activation. [1] Although GPRP can inhibit platelet aggregation, this may limit its potential clinical application value as an antithrombotic drug. [1]
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| Molecular Formula |
C20H35N7O7
|
|---|---|
| Molecular Weight |
485.5346
|
| Exact Mass |
485.259
|
| CAS # |
157009-81-9
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| Related CAS # |
GPRP;67869-62-9
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| PubChem CID |
118986652
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
6
|
| Hydrogen Bond Acceptor Count |
9
|
| Rotatable Bond Count |
9
|
| Heavy Atom Count |
34
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| Complexity |
725
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| Defined Atom Stereocenter Count |
3
|
| SMILES |
CC(=O)O.C1C[C@H](N(C1)C(=O)CN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)O
|
| InChi Key |
ZYTSTPIIKNCGRE-QKWXXBCPSA-N
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| InChi Code |
InChI=1S/C18H31N7O5.C2H4O2/c19-10-14(26)24-8-2-5-12(24)15(27)23-11(4-1-7-22-18(20)21)16(28)25-9-3-6-13(25)17(29)30;1-2(3)4/h11-13H,1-10,19H2,(H,23,27)(H,29,30)(H4,20,21,22);1H3,(H,3,4)/t11-,12-,13-;/m0./s1
|
| Chemical Name |
acetic acid;(2S)-1-[(2S)-2-[[(2S)-1-(2-aminoacetyl)pyrrolidine-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carboxylic 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)
|
| Solubility (In Vitro) |
H2O : ~125 mg/mL (~268.93 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (215.14 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0596 mL | 10.2980 mL | 20.5960 mL | |
| 5 mM | 0.4119 mL | 2.0596 mL | 4.1192 mL | |
| 10 mM | 0.2060 mL | 1.0298 mL | 2.0596 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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