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.
Product information
CAS Number: 124555-18-6
Molecular Weight: 351.36
Formula: C15H21N5O5
Chemical Name: (2S,3R,4S,5R)-2-(6-{[(1S,2S)-2-hydroxycyclopentyl]amino}-9H-purin-9-yl)-5-(hydroxymethyl)oxolane-3,4-diol
Smiles: OC[C@H]1O[C@@H]([C@H](O)[C@@H]1O)N1C=NC2C1=NC=NC=2N[C@H]1CCC[C@@H]1O
InChiKey: GYWXTRVEUURNEW-KOALMESCSA-N
InChi: InChI=1S/C15H21N5O5/c21-4-9-11(23)12(24)15(25-9)20-6-18-10-13(16-5-17-14(10)20)19-7-2-1-3-8(7)22/h5-9,11-12,15,21-24H,1-4H2,(H,16,17,19)/t7-,8-,9+,11+,12+,15-/m0/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : ≥ 100 mg/mL (284.61 mM). H2O : 100 mg/mL (284.61 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
GR79236 inhibits Isoprenaline-stimulated cAMP accumulation in DDT-MF2 cells with an IC50 of 2.6 nM. GR79236 inhibits catecholamine-induced lipolysis in human, rat and dog isolated adipocytes.
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). 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. 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.
Products are for research use only. Not for human use.
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