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GSK2245035

Catalog No. T11482 CAS 1207629-49-9

GSK2245035 is a highly selective intranasal TLR7 agonist with preferential Type-1 interferon (IFN)-stimulating properties (pEC50s: 9.3 and 6.5 for IFNα and TFNα). It effectively suppresses allergen-induced Th2 cytokine production in human peripheral blood cell cultures.

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GSK2245035, CAS 1207629-49-9

Pack Size	Availability	Price/USD
5 mg	8-10 weeks	$ 272.00
25 mg	8-10 weeks	$ 947.00
50 mg	8-10 weeks	$ 1,230.00
100 mg	8-10 weeks	$ 1,640.00
1 mL * 10 mM (in DMSO)	8-10 weeks	$ 298.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

Biological Description

Chemical Properties

Storage & Solubility Information

Description	GSK2245035 is a highly selective intranasal TLR7 agonist with preferential Type-1 interferon (IFN)-stimulating properties (pEC50s: 9.3 and 6.5 for IFNα and TFNα). It effectively suppresses allergen-induced Th2 cytokine production in human peripheral blood cell cultures.
Targets&IC50	TNF-α:6.5(pEC50), IFN-α:9.3(pEC50)
In vitro	In a dose-dependent manner,GSK2245035 (0.01, 0.1, 1, 10, 100, 1000, 10000 nM;?6 days) reduces levels of the Th2 cytokines IL-5 and IL-13 released in response to Timothy grass or house dust mite in human PBMC cultures derived from individuals allergic to these allergens.
In vivo	GSK2245035 (3, 30, 300, 3000 ng/kg; 6 hours) treatment can make plasma IP-10 provided the most sensitive biomarker of target engagement with raised levels of this chemokine detected at doses of 30 ng/kg and above in the cynomolgus monkey.?GSK2245035 (i.n.; 0.03-1 mg/kg; 6 hours) makes dose-related increasing in IFNα levels in serum at doses of 0.3 mg/kg and above at the 2 h time point which had subsided at 6 h.

Molecular Weight	390.52
Formula	C20H34N6O2
CAS No.	1207629-49-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Biggadike K, et al. Discovery of 6-Amino-2-{[(1S)-1-methylbutyl]oxy}-9-[5-(1-piperidinyl)pentyl]-7,9-dihydro-8H-purin-8-one (GSK2245035), a Highly Potent and Selective Intranasal Toll-Like Receptor 7 Agonist for the Treatment of Asthma. J Med Chem. 2016 Mar 10;59(5):1711-26.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

GSK2245035 1207629-49-9 Others GSK-2245035 GSK 2245035 inhibitor inhibit

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