A TLR7 agonist
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GSK2245035

Item No. 33171

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-amino-7,9-dihydro-2-[(1S)-1-methylbutoxy]-9-[5-(1-piperidinyl)pentyl]-8H-purin-8-one
CAS Number
1207629-49-9
Molecular Formula
C20H34N6O2
Formula Weight
390.5
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: 10 mM
SMILES
O=C(N(C1=NC(O[C@@H](C)CCC)=N2)CCCCCN3CCCCC3)NC1=C2N
InChi Code
InChI=1S/C20H34N6O2/c1-3-10-15(2)28-19-23-17(21)16-18(24-19)26(20(27)22-16)14-9-5-8-13-25-11-6-4-7-12-25/h15H,3-14H2,1-2H3,(H,22,27)(H2,21,23,24)/t15-/m0/s1
InChi Key
LFMPVTVPXHNXOT-HNNXBMFYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $134

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    10 mg

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    Cayman Chemical
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    Product Description

    GSK2245035 is a toll-like receptor 7 (TLR7) agonist.1 It selectively induces the production of IFN-α over TNF-α in isolated human peripheral blood mononuclear cells (PBMCs; EC50s = 0.63 and 316 nM, respectively), as well as over the production of TNF-α, IL-1β, IFN-γ, IL-10, and IL-12p70 in isolated human whole blood (EC50s = 63-10,000 nM). GSK2245035 (0.1-1,000 nM) reduces timothy grass- or house dust mite-induced IL-10 and IL-5 release in isolated human PBMCs. Intranasal administration of GSK2245035 (0.03-1 mg/kg) increases serum IP-10 levels, a marker of IFN-α induction, in mice. It also increases serum levels of IP-10 in cynomolgus monkeys.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Biggadike, K., Ahmed, M., Ball, D.I., 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. 59(5), 1711-1726 (2016).