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

GSK2245035 

Cat. No.: HY-118250 Purity: 99.79%
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 asthma.

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

GSK2245035 Chemical Structure

GSK2245035 Chemical Structure

CAS No. : 1207629-49-9

Size Price Stock Quantity
10 mM * 1  mL in DMSO USD 330 In-stock
Estimated Time of Arrival: December 31
5 mg USD 300 In-stock
Estimated Time of Arrival: December 31
10 mg USD 480 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1350 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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 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.
Clinical Trial
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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (320.09 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5607 mL 12.8034 mL 25.6069 mL
5 mM 0.5121 mL 2.5607 mL 5.1214 mL
10 mM 0.2561 mL 1.2803 mL 2.5607 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.33 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (5.33 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (5.33 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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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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HY-118250
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