1. GPCR/G Protein
  2. Adenosine Receptor
  3. GR79236

GR79236 

Cat. No.: HY-18978 Purity: 99.79%
Handling Instructions

GR79236 is a highly potent, selective and orally active adenosine A1 receptor agonist with a Kis of 3.1 nM and 1300 nM for A1 and A2 receptors, respectively. GR79236 has anti-nociceptive and anti-inflammatory actions.

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

GR79236 Chemical Structure

GR79236 Chemical Structure

CAS No. : 124555-18-6

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Free Sample (0.5-1 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 119 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 119 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 108 In-stock
Estimated Time of Arrival: December 31
10 mg USD 144 In-stock
Estimated Time of Arrival: December 31
50 mg USD 576 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

GR79236 is a highly potent, selective and orally active adenosine A1 receptor agonist with a Kis of 3.1 nM and 1300 nM for A1 and A2 receptors, respectively. GR79236 has anti-nociceptive and anti-inflammatory actions[1][2].

IC50 & Target

Ki: 3.1 nM (Adenosine A1 receptor) and 1300 nM (Adenosine A2 receptor)[1]

In Vitro

GR79236 inhibits Isoprenaline-stimulated cAMP accumulation in DDT-MF2 cells with an IC50 of 2.6 nM[1].
GR79236 inhibits catecholamine-induced lipolysis in human, rat and dog isolated adipocytes[3].

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

In Vivo

GR79236 decreases locomotor activity and inhibits DMCM-induced seizures in mice (ED50s of 0.13 mg/kg and 0.3 mg/kg, respectively)[1].
Oral administration of GR79236 (0.1-10 mg/kg) to fed rats induces minimal changes in the plasma concentration of non-esterified fatty acids and in the blood concentrations of glucose and lactate[3].
Intravenous infusion of GR79236 to fasted pithed rats, or oral administration of GR79236 to fasted conscious rats and dogs, produces time- and dose-dependent decreases in the plasma non-esterified fatty acid concentration. In the fasted rats, doses of GR79236 that lowered plasma levels of non-esterified fatty acids also produced hypotriglyceridaemia and anti-ketotic effects[3].

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

Molecular Weight

351.36

Formula

C₁₅H₂₁N₅O₅

CAS No.
SMILES
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: 

H2O : 100 mg/mL (284.61 mM; Need ultrasonic)

DMSO : ≥ 100 mg/mL (284.61 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8461 mL 14.2304 mL 28.4608 mL
5 mM 0.5692 mL 2.8461 mL 5.6922 mL
10 mM 0.2846 mL 1.4230 mL 2.8461 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: ≥ 2.5 mg/mL (7.12 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (7.12 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (7.12 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.79%

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Keywords:

GR79236GR 79236GR-79236Adenosine ReceptorP1 receptorAdenosine-A1anti-nociceptiveanti-inflammatoryseizurescAMP,Inhibitorinhibitorinhibit

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Product Name:
GR79236
Cat. No.:
HY-18978
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