1. GPCR/G Protein
  2. Adenosine Receptor
  3. GP531

GP531 

Cat. No.: HY-U00116 Purity: 98.95%
Handling Instructions

GP531 is a potent, second-generation adenosine regulating agent, is pharmacologically silent under basal conditions but increases localized endogenous adenosine during ischemia.

For research use only. We do not sell to patients.

GP531 Chemical Structure

GP531 Chemical Structure

CAS No. : 142344-87-4

Size Price Stock Quantity
5 mg USD 540 In-stock
Estimated Time of Arrival: December 31
10 mg USD 980 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2800 In-stock
Estimated Time of Arrival: December 31
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200 mg   Get quote  

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Description

GP531 is a potent, second-generation adenosine regulating agent, is pharmacologically silent under basal conditions but increases localized endogenous adenosine during ischemia.

IC50 & Target

Adenosine Receptor[1]

In Vivo

Low-dose GP531 reduces infarct size by 34% compared with vehicle and reduces the extent of the anatomic no-reflow zone by 31% compared with vehicle. Infarct size and zone of no-reflow in the high dose are reduced by 22% and 16%, respectively. GP531 does not affect hemodynamics or blood flow. GP531 is effective at the lower dose in reducing the severity of ischemic/reperfusion injury, without inducing the adverse hemodynamic effects associated with adenosine administration such as bradycardia and hypotension[1]. GP531 infusion has no effect on heart rate or mean aortic pressure but significantly decreases left ventricular end-diastolic pressure, end-diastolic volume, end-systolic volume and end-diastolic wall stress. GP531 significantly increases left ventricular EF, deceleration time of early mitral inflow velocity and the slope of end-systolic PVR without increasing MVO2[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

347.37

Formula

C₁₆H₂₁N₅O₄

CAS No.
SMILES

O=C(C1=C(N)N([[email protected]]2[[email protected]@H]([[email protected]@H]([[email protected]@H](CNCC3=CC=CC=C3)O2)O)O)C=N1)N

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (359.85 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.99 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (5.99 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (5.99 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Animal Administration
[1]

Rabbits: Baseline hemodynamic parameters and temperature are obtained. The rabbits are randomized to 1 of 3 groups: a low dose of GP531, a high dose of GP 531, or vehicle (10% sodium metabisulfite). The low dose consists of a loading dose of 700 mg/kg given over 10 minutes starting at 12 minutes before coronary artery occlusion, followed by an infusion of 10 mg/kg per minute for the duration of the study. The high dose consists of a loading dose of 2100 mg/kg given over 10 minutes starting at 12 minutes before CAO followed by an infusion of 30 mg/kg per min for the duration of the study. All rabbits receive the same volume (12 mL over the duration of the study), so the concentrations are adjusted for body weight. The rabbits are then subjected to 30 minutes of coronary artery occlusion. The coronary artery is occluded by tightening the snare. Regional myocardial blood flow is measured during the ischemic period at 25 minutes of CAO[1].

Dog: Six dogs with intracoronary microembolizationinduced HF receive a constant intravenous infusion of GP531 (10 μg/kg/min) or vehicle (normal saline) for 6 h in random order 1 week apart. Hemodynamic measurements are made at baseline and at 1, 2, 3, 4, 5 and 6 h after initiating drug infusion. Myocardial oxygen consumption (MVO2) is measured at baseline and 4 and 6 h. LV pressure-volume relationship (PVR) is measured at baseline and 6 h[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

GP531GP 531GP-531Adenosine ReceptorP1 receptorInhibitorinhibitorinhibit

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