| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
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| ln Vitro |
GR79236 suppresses the buildup of cAMP induced by isoproterenol in DDT-MF2 cells, with an IC50 of 2.6 nM [1]. In isolated adipocytes from humans, rats, and dogs, GR79236 suppresses catecholamine-induced lipolysis [3].
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| ln Vivo |
In mice, GR79236 suppresses seizures caused by DMCM and decreases locomotor activity (ED50 = 0.13 mg/kg and 0.3 mg/kg, respectively) [1]. Oral treatment of GR79236 (0.1–10 mg/kg) to fed rats has the potential to slightly alter blood glucose and lactate concentrations as well as plasma non-esterified fatty acid concentrations [3]. The amounts of plasma nonesterified fatty acids were shown to decrease in a time- and dose-dependent manner in rats that were fasted or in dogs that were given GR79236 orally. Doses of GR79236 that lower non-esterified fatty acid plasma levels in fasting rats also cause hypotriglyceridemia and antiketogenic effects [3].
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| References |
[1]. L J Knutsen, et al. N-substituted adenosines as novel neuroprotective A(1) agonists with diminished hypotensive effects. J Med Chem. 1999 Sep 9;42(18):3463-77.
[2]. Sneyd JR, et al. Multicentre evaluation of the adenosine agonist GR79236X in patients with dental pain after third molar extraction. Br J Anaesth. 2007 May;98(5):672-676. [3]. P Strong, et al. Suppression of non-esterified fatty acids and triacylglycerol in experimental animals by the adenosine analogue GR79236. Clin Sci (Lond). 1993 Jun;84(6):663-9. |
| Additional Infomation |
(2R,3R,4S,5R)-2-[6-[[(1S,2S)-2-hydroxycyclopentyl]amino]-9-purinyl]-5-(hydroxymethyl)oxolane-3,4-diol is a purine nucleoside.
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| Molecular Formula |
C15H21N5O5
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|---|---|
| Molecular Weight |
351.36
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| Exact Mass |
351.154
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| CAS # |
124555-18-6
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| PubChem CID |
9884817
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.89g/cm3
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| Boiling Point |
728.3ºC at 760mmHg
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| Flash Point |
394.3ºC
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| Vapour Pressure |
0mmHg at 25°C
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| Index of Refraction |
1.846
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| LogP |
-0.1
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
25
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| Complexity |
474
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| Defined Atom Stereocenter Count |
6
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| 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
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| InChi Key |
GYWXTRVEUURNEW-TVDBPQCTSA-N
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| InChi Code |
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
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| Chemical Name |
(2R,3R,4S,5R)-2-[6-[[(1S,2S)-2-hydroxycyclopentyl]amino]purin-9-yl]-5-(hydroxymethyl)oxolane-3,4-diol
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| Synonyms |
GR 79236; GR-79236; GR79236
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ~100 mg/mL (~284.61 mM)
DMSO : ≥ 100 mg/mL (~284.61 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.12 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.12 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.12 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 11.11 mg/mL (31.62 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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