[CAS NO. 124555-18-6] GR79236

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PRODUCTS SPECIFICATIONS [124555-18-6]

Catalog

HY-18978

Brand

MCE

CAS

124555-18-6

DESCRIPTION [124555-18-6]

Overview

MDL	-
Molecular Weight	351.36
Molecular Formula	C15H21N5O5
SMILES	OC[C@@H]1[C@H]([C@H]([C@H](N2C=NC3=C2N=CN=C3N[C@@H]4[C@@H](O)CCC4)O1)O)O

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

Summary

GR79236 is a highly potent, selective and orally active adenosine A1 receptor agonist with a K _i s 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 IC ₅₀ 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 (ED ₅₀ s 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.

Appearance

Solid

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:

H ₂ O : 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: PBS

Solubility: 11.11 mg/mL (31.62 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
2.

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
3.

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
4.

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 available by MCE.