| 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 |
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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].
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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 |
| Molecular Formula |
C16H21N5O4
|
|---|---|
| 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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