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

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

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GP531 Chemical Structure

GP531 Chemical Structure

CAS No. : 142344-87-4

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 594 In-stock
Solution
10 mM * 1 mL in DMSO USD 594 In-stock
Solid
5 mg USD 540 In-stock
10 mg USD 980 In-stock
50 mg USD 2800 In-stock
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GP531 Related Antibodies

Top Publications Citing Use of Products

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Adenosine A1 receptor (A1R) Adenosine A2A receptor (A2AR) Adenosine A2B receptor (A2BR) Adenosine A3 receptor (A3R)

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

347.37

Formula

C16H21N5O4
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(C1=C(N)N([C@H]2[C@@H]([C@@H]([C@@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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8788 mL 14.3939 mL 28.7877 mL 71.9694 mL
5 mM 0.5758 mL 2.8788 mL 5.7575 mL 14.3939 mL
10 mM 0.2879 mL 1.4394 mL 2.8788 mL 7.1969 mL
15 mM 0.1919 mL 0.9596 mL 1.9192 mL 4.7980 mL
20 mM 0.1439 mL 0.7197 mL 1.4394 mL 3.5985 mL
25 mM 0.1152 mL 0.5758 mL 1.1515 mL 2.8788 mL
30 mM 0.0960 mL 0.4798 mL 0.9596 mL 2.3990 mL
40 mM 0.0720 mL 0.3598 mL 0.7197 mL 1.7992 mL
50 mM 0.0576 mL 0.2879 mL 0.5758 mL 1.4394 mL
60 mM 0.0480 mL 0.2399 mL 0.4798 mL 1.1995 mL
80 mM 0.0360 mL 0.1799 mL 0.3598 mL 0.8996 mL
100 mM 0.0288 mL 0.1439 mL 0.2879 mL 0.7197 mL
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GP531 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GP531142344-87-4GP 531GP-531Adenosine ReceptorP1 receptorInhibitorinhibitorinhibit

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