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GSK2245035

Cat. No. M10824
GSK2245035 Structure
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Biological Activity

GSK2245035 is a highly potent, selective intranasal Toll-Like receptor 7 (TLR7) agonist with preferential stimulation of interferon type 1 (IFN). GSK2245035 for IFNα and TNFα pEC50 9.3 and 6.5, respectively. GSK2245035 effectively inhibits allergen-induced Th2 cytokine production in human peripheral blood cell cultures. GSK2245035 has the potential for asthma.

Chemical Information
Molecular Weight 390.52
Formula C20H34N6O2
CAS Number 1207629-49-9
Solubility (25°C) DMSO ≥ 100 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] L M Posobiec, et al. J Reprod Immunol. GSK2245035, a TLR7 agonist, Does Not Increase Pregnancy Loss in Cynomolgus Monkeys

[2] Hilary Siddall, et al. PLoS One. Intranasal GSK2245035, a Toll-like receptor 7 agonist, does not attenuate the allergen-induced asthmatic response in a randomized, double-blind, placebo-controlled experimental medicine study

[3] A K Ellis, et al. Clin Exp Allergy. Safety and pharmacodynamics of intranasal GSK2245035, a TLR7 agonist for allergic rhinitis: A randomized trial

[4] Keith Biggadike, et al. J Med Chem. 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

[5] D Tsitoura, et al. Clin Pharmacol Ther. Early clinical evaluation of the intranasal TLR7 agonist GSK2245035: Use of translational biomarkers to guide dosing and confirm target engagement

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Keywords: GSK2245035 supplier, TLR, inhibitors, activators

 
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