| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
GP531 acts as an adenosine regulating agent that increases concentrations of endogenous adenosine, a natural cardioprotective agent. Unlike direct adenosine receptor agonists, ARAs like GP531 are pharmacologically silent under normal conditions but selectively increase adenosine levels in ischemic tissues. This mechanism provides cardioprotection during ischemia without causing systemic side effects associated with direct adenosine administration.
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| ln Vitro |
In vitro, GP531 exhibits adenosine-regulating activity by increasing localized adenosine concentrations during ischemic conditions. The compound is pharmacologically silent under basal conditions, meaning it does not significantly affect adenosine levels in normoxic tissues. Detailed IC₅0 or EC₅0 values are not extensively documented in the available literature. The compound's activity is measured by its ability to increase adenosine production in ischemic cells.
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| ln Vivo |
In comparison to vehicle, low-dose GP531 decreased the extent of the anatomic no-reflow zone by 31% and the size of the infarct by 34%. The no-reflow area and infarct size were lowered by 16% and 22%, respectively, at high dosages. Blood flow or hemodynamics are unaffected by GP531. Even at lesser dosages, GP531 is useful in lessening the severity of ischemia/reperfusion injury without producing the negative hemodynamic consequences of adenosine treatment, such as bradycardia and hypotension [1]. Heart rate and mean aortic pressure were unaffected by GP531 infusion, but end-diastolic pressure, end-diastolic volume, end-systolic volume, and end-diastolic wall stress in the left ventricle were all markedly decreased. Without raising MVO2, GP531 dramatically raises end-systolic PVR slope, left ventricular EF, and the deceleration duration of early mitral inflow velocity [2].
In vivo, GP531 is a second-generation adenosine regulating agent with anti-ischemic properties. It increases localized endogenous adenosine during ischemia, providing cardioprotection without affecting systemic adenosine levels. The compound is pharmacologically silent under basal conditions but activates during ischemic stress. Further in vivo efficacy studies in animal models of myocardial ischemia would be needed to fully characterize its therapeutic potential. |
| Enzyme Assay |
The in vitro adenosine-regulating assay measures adenosine production in cells or tissues under normoxic and ischemic conditions. Cells are incubated with GP531 at various concentrations, and extracellular adenosine levels are measured by HPLC or mass spectrometry. The compound's activity is assessed by its ability to increase adenosine production specifically during ischemic stress. The assay distinguishes between basal and ischemia-induced adenosine production to confirm the compound's "silent" profile under normal conditions.
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| Cell Assay |
For in vitro cell-based assays, cardiomyocytes or other relevant cell types are cultured and subjected to normoxic or ischemic conditions (such as hypoxia or glucose deprivation). GP531 is added at various concentrations during the stress period. Adenosine levels in the culture medium are quantified by HPLC, mass spectrometry, or enzymatic assays. Cell viability is assessed to confirm that the compound is not cytotoxic. Experiments are typically performed in triplicate.
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| Animal Protocol |
In vivo animal studies for GP531 typically involve rodent or canine models of myocardial ischemia (such as coronary artery ligation). The compound is administered intravenously or orally prior to or during the ischemic event. Infarct size is measured by histochemical staining (TTC staining). Cardiac function is assessed by echocardiography or hemodynamic monitoring. Adenosine levels in cardiac tissue or coronary sinus blood are measured to confirm target engagement. Survival and recovery are monitored.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of GP531 are not extensively documented in the available literature. The compound has molecular weight 347.37 and molecular formula C1₆H21N₅O4. The chemical name is 5-amino-1-[(2R,3R,4S,5R)-5-[(benzylamino)methyl]-3,4-dihydroxyoxolan-2-yl]-1H-imidazole-4-carboxamide. Purity is typically ≥98%. Further PK parameters would require dedicated studies.
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| Toxicity/Toxicokinetics |
*Toxicological data for GP531 are not well characterized in the public domain. As a research chemical, standard safety precautions should be observed. The compound is for laboratory use only and not intended for human therapeutic applications. Adenosine regulating agents are generally considered to have favorable safety profiles due to their "silent" mechanism under basal conditions. Comprehensive toxicity profiling would be required for therapeutic development.
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| References |
[1]. Hale SL, et al. Cardioprotection with adenosine-regulating agent, GP531: effects on no-reflow, infarct size, and blood flow following ischemia/ reperfusion in the rabbit. J Cardiovasc Pharmacol Ther. 2010 Mar;15(1):60-7.
[2]. Wang M, et al. Acute intravenous infusion of an adenosine regulating agent improves left ventricular function in dogs with advanced heart failure. Cardiovasc Drugs Ther. 2013 Dec;27(6):489-98 |
| Additional Infomation |
GP531 (CAS# 142344-87-4) is a second-generation adenosine regulating agent with anti-ischemic properties. It is structurally similar to acadesine and is used in cardiovascular research. The compound is pharmacologically silent under basal conditions but increases endogenous adenosine during ischemia. It is not approved for clinical use and is strictly for laboratory research purposes.
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| Molecular Formula |
C16H21N5O4
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|---|---|
| Molecular Weight |
347.369043111801
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| Exact Mass |
347.159
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| CAS # |
142344-87-4
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| PubChem CID |
164444
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.6g/cm3
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| Boiling Point |
703.1ºC at 760mmHg
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| Flash Point |
379ºC
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| Vapour Pressure |
9.55E-21mmHg at 25°C
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| Index of Refraction |
1.729
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| LogP |
0.829
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
25
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| Complexity |
462
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| Defined Atom Stereocenter Count |
4
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| SMILES |
O1[C@H]([C@@H]([C@@H]([C@H]1CNCC1C=CC=CC=1)O)O)N1C=NC(C(N)=O)=C1N
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| InChi Key |
LECUGLHMNZTZQB-XNIJJKJLSA-N
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| InChi Code |
InChI=1S/C16H21N5O4/c17-14-11(15(18)24)20-8-21(14)16-13(23)12(22)10(25-16)7-19-6-9-4-2-1-3-5-9/h1-5,8,10,12-13,16,19,22-23H,6-7,17H2,(H2,18,24)/t10-,12-,13-,16-/m1/s1
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| Chemical Name |
5-amino-1-[(2R,3R,4S,5R)-5-[(benzylamino)methyl]-3,4-dihydroxyoxolan-2-yl]imidazole-4-carboxamide
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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 |
| 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) |
DMSO : ~125 mg/mL (~359.85 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.99 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.99 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.99 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8788 mL | 14.3939 mL | 28.7877 mL | |
| 5 mM | 0.5758 mL | 2.8788 mL | 5.7575 mL | |
| 10 mM | 0.2879 mL | 1.4394 mL | 2.8788 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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