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GSK-256066
CAS No. 801312-28-7
GSK-256066( GSK256066 | GSK 256066 )
Catalog No. M16000 CAS No. 801312-28-7
A potent, selective PDE4 inhibitor with pIC50 of 11.5, 11.3, 11.4, and 11.9 for PDE4B, A, C, and D, respectively.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 2MG | 42 | Get Quote |
|
| 5MG | 68 | Get Quote |
|
| 10MG | 115 | Get Quote |
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| 25MG | 237 | Get Quote |
|
| 50MG | 385 | Get Quote |
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| 100MG | Get Quote | Get Quote |
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| 200MG | Get Quote | Get Quote |
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| 500MG | Get Quote | Get Quote |
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| 1G | Get Quote | Get Quote |
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Biological Information
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Product NameGSK-256066
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NoteResearch use only, not for human use.
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Brief DescriptionA potent, selective PDE4 inhibitor with pIC50 of 11.5, 11.3, 11.4, and 11.9 for PDE4B, A, C, and D, respectively.
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DescriptionA potent, selective PDE4 inhibitor with pIC50 of 11.5, 11.3, 11.4, and 11.9 for PDE4B, A, C, and D, respectively; displays >380,000-fold selectivity over PDE1/2/3/5/6/7; inhibits TNFα production by lLPS-stimulated human peripheral blood monocytes with IC50 of 0.01 nM; inhibites LPS-induced pulmonary neutrophilia with ED50 of 1.1 ug/kg (aqueous suspension) and 2.9 ug/kg (dry powder formulation) in rats.COPD Phase 2 Discontinued.
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In Vitro——
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In VivoAnimal Model:Male Brown Norway rats (180-200 g)Dosage:10 μg/kg Administration:Intratracheal injection; before (36 hours, 24 hours, 18 hours, 12 hours, 6 hours, and 2 hours) and after (0 hour, 2 hours) LPS challenge Result:Inhibited the LPS-induced pulmonary neutrophilia.
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SynonymsGSK256066 | GSK 256066
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PathwayAngiogenesis
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TargetPDE
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RecptorPDE4B
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Research AreaInflammation/Immunology
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IndicationCOPD
Chemical Information
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CAS Number801312-28-7
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Formula Weight518.5842
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Molecular FormulaC27H26N4O5S
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Purity>98% (HPLC)
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SolubilityDMSO: ≥ 5.2 mg/mL
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SMILESCC1=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
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Chemical Name3-Quinolinecarboxamide, 6-[[3-[(dimethylamino)carbonyl]phenyl]sulfonyl]-4-[(3-methoxyphenyl)amino]-8-methyl-
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Woodrow MD, et al. Bioorg Med Chem Lett. 2009 Sep 1;19(17):5261-5.
2. Tralau-Stewart CJ, et al. J Pharmacol Exp Ther. 2011 Apr;337(1):145-54.
3. Nials AT, et al. J Pharmacol Exp Ther. 2011 Apr;337(1):137-44.
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