| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
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| ln Vitro |
In membranes made from Chinese hamster experimental cells expressing recombinant human HCA2, GSK256073 is about ten times more potent than nicotinic acid against human HCA2 (pEC50 value of 7.5 compared to 6.7 for nicotinic acid), with a good activity value of 6.9 compared to the HCA2 proportional ortholog (pEC50) acid 6.4 [2]. Using the primary adipocyte kit, propylene glycol isoform (100 nM) is converted to GSK256073 (100 μM) [2].
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|---|---|
| ln Vivo |
NEFA recovery began quickly in topology when GSK256073 (sidewall; 1, 30, and 100 mg/kg) was administered; peak dose-related inhibition rates were 74%, 81%, and 88%, respectively. Even though the pattern of triglyceride reduction was longer, 91% of the reduction was still evident 6 hours after 10 mg/kg [2]. GSK256073 (IV; 1–10 mg/kg) decreases NEFA in a dose-related manner. ear temperature increased by 40% when 10 mg/kg iv niacin and 10 mg/kg iv GSK256073 were administered intravenously [2].
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| Animal Protocol |
Animal/Disease Models: SD rat [2]
Doses: 1, 30 and 100 mg/kg Route of Administration: Oral administration Experimental Results: Inhibited NEFA expression in a dose-dependent manner. Animal/Disease Models: guinea pig [2] Doses: 10 mg/kg Route of Administration: intravenous (iv) (iv)injection Experimental Results: It has the anti-lipolysis and flushing effects of HCA2 agonist. |
| References |
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| Molecular Formula |
C10H13CLN4O2
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|---|---|
| Molecular Weight |
256.69
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| Exact Mass |
256.073
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| CAS # |
862892-90-8
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| Related CAS # |
1228650-42-7 (tris);862892-90-8 (free);
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| PubChem CID |
46215799
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| Appearance |
White to off-white solid powder
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| LogP |
1.668
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
17
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| Complexity |
325
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
CGAMDQCXAAOFSR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H13ClN4O2/c1-2-3-4-5-15-7-6(12-9(11)13-7)8(16)14-10(15)17/h2-5H2,1H3,(H,12,13)(H,14,16,17)
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| Chemical Name |
8-chloro-3-pentyl-7H-purine-2,6-dione
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| Synonyms |
GSK-256073; GSK 256073; GSK256073
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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) |
DMSO : ~16.67 mg/mL (~64.94 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.67 mg/mL (6.51 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 16.7 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.8957 mL | 19.4787 mL | 38.9575 mL | |
| 5 mM | 0.7791 mL | 3.8957 mL | 7.7915 mL | |
| 10 mM | 0.3896 mL | 1.9479 mL | 3.8957 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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