1. Immunology/Inflammation
    Apoptosis
  2. Toll-like Receptor (TLR)
    IFNAR
    TNF Receptor
  3. GSK2245035

GSK2245035 

Cat. No.: HY-118250
Handling Instructions

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 the treatment of asthma.

For research use only. We do not sell to patients.

GSK2245035 Chemical Structure

GSK2245035 Chemical Structure

CAS No. : 1207629-49-9

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Description

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 the treatment of asthma[1].

IC50 & Target[1]

TLR7

 

IFNα

9.3 (pEC50)

TNFα

6.5 (pEC50)

In Vitro

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 a dose-dependent manner[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].
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.
Molecular Weight

390.52

Formula

C₂₀H₃₄N₆O₂

CAS No.

1207629-49-9

SMILES

O=C1NC2=C(N=C(N=C2N1CCCCCN3CCCCC3)O[[email protected]](CCC)C)N

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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

GSK2245035GSK 2245035GSK-2245035Toll-like Receptor (TLR)IFNARTNF ReceptorInterferon-α/β receptorInterferon-alpha/beta receptor Tumor Necrosis Factor ReceptorTNFRintranasalpreferentialType-1interferonallergen-inducedTh2cytokineperipheralbloodasthmaInhibitorinhibitorinhibit

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GSK2245035
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