| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| 500mg |
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| ln Vitro |
GSK256073 exhibits good activity in membranes prepared from Chinese hamster ovary cells expressing recombinant human HCA2 and is about ten times more potent than niacin against human HCA2 (pEC50 value of 7.5 compared to 6.7 for niacin) and the rat ortholog of HCA2 (pEC50 6.9, and niacin 6.4). In rat primary adipocytes, 100 μM of GSK256073 is inhibited by 100 nM of isoproterenol [2].
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| ln Vivo |
Rats administered GSK256073 orally at doses of 1, 30, and 100 mg/kg showed a quick start to the reduction of NEFA, with maximum dose-related inhibition rates of 74%, 81%, and 88%, respectively. Although it took longer, triglycerides also reduced in a similar manner, with a 91% reduction remaining at 6 hours following a dose of 10 mg/kg [2]. GSK256073 (IV; 1–10 mg/kg) decreases NEFA in a dose-related manner. But only 40% of the elevation in ear temperature brought on by 10 mg/kg iv niacin was brought on by 10 mg/kg iv GSK256073 [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 as a dose-dependent manner. Animal/Disease Models: Guinea pigs[2] Doses: 10 mg/kg Route of Administration: intravenous (iv) injection Experimental Results: Had the antilipolytic and flushing effects as a HCA2 agonist. |
| References |
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| CAS # |
802892-90-8
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|---|---|
| Appearance |
White to off-white solid powder
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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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