| Identification | Back Directory | [Name]
GSK2245035 | [CAS]
1207629-49-9 | [Synonyms]
GSK2245035
GSK2245035
(GSK 2245035 | [EINECS(EC#)]
629-855-3 | [Molecular Formula]
C20H34N6O2 | [MDL Number]
MFCD32008232 | [MOL File]
1207629-49-9.mol | [Molecular Weight]
390.52 |
| Chemical Properties | Back Directory | [density ]
1.142±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: 125 mg/mL (320.09 mM) | [form ]
A solid | [pka]
10.28±0.20(Predicted) | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Uses]
GSK2245035 is a highly potent and selective intranasal Toll-Like receptor 7 (TLR7) agonist with preferential Type-1 interferon (IFN)-stimulating properties. GSK2245035 has pEC50s of 9.3 and 6.5 for IFNα and TFNα. GSK2245035 effectively suppresses allergen-induced Th2 cytokine production in human peripheral blood cell cultures. GSK2245035 is used for asthma[1]. | [in vivo]
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[1].
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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[1].
| Animal Model: | Female BALB/c mice[1] | | Dosage: | 0.03, 0.1, 0.3, 1 mg/kg | | Administration: | Intranasally (i.n.); 6 hours | | Result: | Dose-related increases in IFNα levels in serum were detected at doses of 0.3 mg/kg and above at the 2 h time point which had subsided at 6 h.
|
| [IC 50]
TLR7; IFNα: 9.3 (pEC50); CD40: 6.5 (pEC50) | [storage]
Store at -20°C | [References]
[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 M DOI:10.1021/acs.jmedchem.5b01647 |
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| Company Name: |
BOC Sciences
|
| Tel: |
16314854226 |
| Website: |
www.bocsci.com |
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