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Testing Data (GSK256066 is an exceptionally high affinity and selective PDE4 inhibitor with an IC50 of 3.2 pM for PDE4B. GSK256066 suppressed tumor necrosis factor alpha production by lipopolysaccharide (LPS)-stimulated human peripheral blood monocytes with 0.01 nM IC50 (compared with IC50 values of 5, 22, and 389 nM for roflumilast, tofimilast, and cilomilast, respectively) and by LPS-stimulated whole blood with 126 pM IC50. GSK256066 also inhibited LPS-induced increases in exhaled nitric oxide (ED50=35 ug/kg). In addition, GSK256066 prevented pulmonary eosinophilia in rats exposed to ovalbumin (ED50=0.4 ug/kg). In ferrets, inhaled GSK256066 inhibited LPS-induced pulmonary neutrophilia (ED50=18 ug/kg) and no emetic episodes were observed. [1][2])

GSK256066, inhibitor

GSK256066

Synonyms
GSK256066; inhibitor
Ordering
For Research Use Only!
Solubility
DMSO >=5 mg/mL - Water <1 mg/mL - Ethanol <1 mg/mL
Formula
C27H26N4O5S
CAS Number
801312-28-7
Preparation and Storage
Stable for; 2 years at -20 degree C Powder
1 week -4 degree C in DMSO
1 month -80 degree C in DMSO

Testing Data

(GSK256066 is an exceptionally high affinity and selective PDE4 inhibitor with an IC50 of 3.2 pM for PDE4B. GSK256066 suppressed tumor necrosis factor alpha production by lipopolysaccharide (LPS)-stimulated human peripheral blood monocytes with 0.01 nM IC50 (compared with IC50 values of 5, 22, and 389 nM for roflumilast, tofimilast, and cilomilast, respectively) and by LPS-stimulated whole blood with 126 pM IC50. GSK256066 also inhibited LPS-induced increases in exhaled nitric oxide (ED50=35 ug/kg). In addition, GSK256066 prevented pulmonary eosinophilia in rats exposed to ovalbumin (ED50=0.4 ug/kg). In ferrets, inhaled GSK256066 inhibited LPS-induced pulmonary neutrophilia (ED50=18 ug/kg) and no emetic episodes were observed. [1][2])

Testing Data (GSK256066 is an exceptionally high affinity and selective PDE4 inhibitor with an IC50 of 3.2 pM for PDE4B. GSK256066 suppressed tumor necrosis factor alpha production by lipopolysaccharide (LPS)-stimulated human peripheral blood monocytes with 0.01 nM IC50 (compared with IC50 values of 5, 22, and 389 nM for roflumilast, tofimilast, and cilomilast, respectively) and by LPS-stimulated whole blood with 126 pM IC50. GSK256066 also inhibited LPS-induced increases in exhaled nitric oxide (ED50=35 ug/kg). In addition, GSK256066 prevented pulmonary eosinophilia in rats exposed to ovalbumin (ED50=0.4 ug/kg). In ferrets, inhaled GSK256066 inhibited LPS-induced pulmonary neutrophilia (ED50=18 ug/kg) and no emetic episodes were observed. [1][2])
Related Product Information for GSK256066, inhibitor
GSK256066 is an exceptionally high affinity and selective PDE4 inhibitor with an IC50 of 3.2 pM for PDE4B. GSK256066 suppressed tumor necrosis factor alpha production by lipopolysaccharide (LPS)-stimulated human peripheral blood monocytes with 0.01 nM IC50 (compared with IC50 values of 5, 22, and 389 nM for roflumilast, tofimilast, and cilomilast, respectively) and by LPS-stimulated whole blood with 126 pM IC50. GSK256066 also inhibited LPS-induced increases in exhaled nitric oxide (ED50=35 ug/kg). In addition, GSK256066 prevented pulmonary eosinophilia in rats exposed to ovalbumin (ED50=0.4 mug/kg). In ferrets, inhaled GSK256066 inhibited LPS-induced pulmonary neutrophilia (ED50=18 mug/kg) and no emetic episodes were observed. [1][2]

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Product Notes

The GSK256066 (Catalog #AAA8506525) is an Inhibitor and is intended for research purposes only. The product is available for immediate purchase. It is sometimes possible for the material contained within the vial of "GSK256066, Inhibitor" to become dispersed throughout the inside of the vial, particularly around the seal of said vial, during shipment and storage. We always suggest centrifuging these vials to consolidate all of the liquid away from the lid and to the bottom of the vial prior to opening. Please be advised that certain products may require dry ice for shipping and that, if this is the case, an additional dry ice fee may also be required.

Precautions

All products in the AAA Biotech catalog are strictly for research-use only, and are absolutely not suitable for use in any sort of medical, therapeutic, prophylactic, in-vivo, or diagnostic capacity. By purchasing a product from AAA Biotech, you are explicitly certifying that said products will be properly tested and used in line with industry standard. AAA Biotech and its authorized distribution partners reserve the right to refuse to fulfill any order if we have any indication that a purchaser may be intending to use a product outside of our accepted criteria.

Disclaimer

Though we do strive to guarantee the information represented in this datasheet, AAA Biotech cannot be held responsible for any oversights or imprecisions. AAA Biotech reserves the right to adjust any aspect of this datasheet at any time and without notice. It is the responsibility of the customer to inform AAA Biotech of any product performance issues observed or experienced within 30 days of receipt of said product. To see additional details on this or any of our other policies, please see our Terms & Conditions page.

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