GSK2245035( GSK 2245035 | GSK-2245035 )

Catalog No. M10768 CAS No. 1207629-49-9

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

GSK2245035
Note

Research use only, not for human use.
Brief Description

GSK2245035 is a highly potent, selective TLR7 agonist that selectively induces TFN-α in PBMC assays with pEC50 of 9.3, >2 logs selectivity over TNFα pEC50.
Description

GSK2245035 is a highly potent, selective TLR7 agonist that selectively induces TFN-α in PBMC assays with pEC50 of 9.3, >2 logs selectivity over TNFα pEC50; suppresses Th2 cytokine responses to allergens in human cell cultures, causes local upregulation of TLR7-mediated cytokines (IP-10) in vivo after intranasal administration at very low doses.Asthma Phase 2 Clinical.
In Vitro

——
In Vivo

Animal Model:Female BALB/c mice 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.
Synonyms

GSK 2245035 | GSK-2245035
Pathway

Immunology/Inflammation
Target

TLR
Recptor

TLR
Research Area

Inflammation/Immunology
Indication

Asthma

CAS Number

1207629-49-9
Formula Weight

390.532
Molecular Formula

C20H34N6O2
Purity

>98% (HPLC)
Solubility

In Vitro:?DMSO : 125 mg/mL (320.09 mM)
SMILES

CCCC(C)OC1=NC(=C2C(=N1)N(C(=O)N2)CCCCCN3CCCCC3)N
Chemical Name

(S)-6-amino-2-(pentan-2-yloxy)-9-(5-(piperidin-1-yl)pentyl)-7,9-dihydro-8H-purin-8-one

1. Biggadike K, et al. J Med Chem. 2016 Mar 10;59(5):1711-26. 2. Ellis AK, et al. Clin Exp Allergy. 2017 Sep;47(9):1193-1203.

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