1207629-49-9
1207629-49-9 structure
- Name: GSK2245035
- Chemical Name: GSK2245035
- CAS Number: 1207629-49-9
- Molecular Formula: C20H34N6O2
- Molecular Weight: 390.523
- Catalog: Signaling Pathways Immunology/Inflammation IFNAR
- Create Date: 2018-07-03 20:03:12
- Modify Date: 2024-01-10 12:14:31
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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].
| Name | GSK2245035 |
|---|---|
| Synonyms |
6-Amino-2-(2-pentanyloxy)-9-[5-(1-piperidinyl)pentyl]-7,9-dihydro-8H-purin-8-one
8H-Purin-8-one, 6-amino-7,9-dihydro-2-(1-methylbutoxy)-9-[5-(1-piperidinyl)pentyl]- Gsk-2245035 |
| 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]. |
|---|---|
| Related Catalog | |
| Target |
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. |
| References |
| Density | 1.1±0.1 g/cm3 |
|---|---|
| Molecular Formula | C20H34N6O2 |
| Molecular Weight | 390.523 |
| Exact Mass | 390.274323 |
| LogP | 3.37 |
| Index of Refraction | 1.555 |