| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
|
GSK256066 Trifluoroacetate (GSK256066; GSK-256066), the trifluoroacetic acid salt form of GSK256066, is a novel selective
inhibitor of PDE4B (phosphodiesterase 4B) with important biological
activity (e.g. inhibiting pulmonary neutrophilia) and thus has the potential to be used for treatment for chronic obstructive pulmonary disease. It inhibits PDE4B with an IC50 of 3.2 pM, and shows >380,000-fold
selectivity for PDE4B over PDE1/2/3/5/6.
| ln Vitro |
GSK256066 trifluoroacetate has a very high affinity PDE4 inhibitor that is intended for inhalation [1]. GSK256066 trifluoroacetate inhibits PDE4 with the same affinity Subtype AD and is highly selective for PDE4, with >380,000-fold selectivity relative to PDE1/2/3/5/6 and >2500-fold selectivity relative to PDE7[1]. With an IC50 of 0.01 nM, GSK256066 Trifluacetate prevents human peripheral blood mononuclear cells stimulated by lipopolysaccharide (LPS) from producing tumor necrosis factor α[1].
|
|---|---|
| ln Vivo |
GSK256066 trifluoroacetate (0.3-100 μg/kg; intratracheal) in a rat model of acute lung inflammation generated by lipopolysaccharide (LPS) and ovalbumin (OVA) decreases bronchoalveolar perfusion in a dose-dependent manner. An increase in the washout's (BAL) eosinophil count. [2]. LPS-induced pulmonary neutrophilia is inhibited by GSK256066 trifluoroacetate, and ferrets did not exhibit any episodes of emesis [2].
|
| Animal Protocol |
Animal/Disease Models: Male brown Norway rat (180-200 g) [2]
Doses: 0.3-100 μg/kg Route of Administration: intratracheal; 30 minutes before and 6 hrs (hrs (hours)) after ovalbumin challenge Experimental Results: Dose-dependent way to inhibit the increase in the number of eosinophils in BAL. |
| References |
[1]. Tralau-Stewart CJ, et al. GSK256066, an exceptionally high-affinity and selective inhibitor of phosphodiesterase 4 suitable for administration by inhalation: in vitro, kinetic, and in vivo characterization. J Pharmacol Exp Ther, 2011, 337(1), 145-154.
[2]. Nials AT, et al. In vivo characterization of GSK256066, a high-affinity inhaled phosphodiesterase 4 inhibitor. J Pharmacol Exp Ther, 2011, 337(1), 137-144. |
| Molecular Formula |
C₂₉H₂₇F₃N₄O₇S
|
|---|---|
| Molecular Weight |
632.61
|
| CAS # |
1415560-64-3
|
| Related CAS # |
GSK256066;801312-28-7
|
| SMILES |
CC1=CC(=CC2=C(C(=CN=C12)C(=O)N)NC3=CC(=CC=C3)OC)S(=O)(=O)C4=CC=CC(=C4)C(=O)N(C)C.C(=O)(C(F)(F)F)O
|
| Chemical Name |
3-Quinolinecarboxamide, 6-[[3-[(dimethylamino)carbonyl]phenyl]sulfonyl]-4-[(3-methoxyphenyl)amino]-8-methyl-, 2,2,2-trifluoroacetate (1
|
| Synonyms |
GSK256066 GSK-256066 GSK 256066 2,2,2-trifluoroacetic acid
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~25 mg/mL (~39.52 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.95 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 (3.95 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5808 mL | 7.9038 mL | 15.8075 mL | |
| 5 mM | 0.3162 mL | 1.5808 mL | 3.1615 mL | |
| 10 mM | 0.1581 mL | 0.7904 mL | 1.5808 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
