| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| G656495-1ml |
1ml |
期货  |
|
| 规格或纯度 | Moligand™, 10mM in DMSO |
|---|---|
| 英文名称 | GSK2245035 |
| 生化机理 | GSK2245035 是一种高效、选择性鼻内 Toll-Like 受体 7 (TLR7) 激动剂，具有优先刺激 1 型干扰素 (IFN) 的特性。GSK2245035 对 IFNα 和 TFNα 的 pEC 50 s 分别为 9.3 和 6.5。GSK2245035 可有效抑制过敏性疾病的发生。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 激动剂 |
| 作用机制 | Toll 样受体 7 激动剂 |
| 产品介绍 |
GSK2245035 是一种高效的，选择性的鼻内 Toll-Like 受体 7 (TLR7) 激动剂，具有优先刺激 1 型干扰素 (IFN) 的特性。GSK2245035 对 IFNα 和TNFα 的 pEC50 分别为 9.3 和 6.5。GSK2245035 有效抑制人外周血细胞培养物中过敏原诱导的 Th2 细胞因子产生。GSK2245035 有用于哮喘的潜力。 GSK2245035 is a highly potent and selective intranasal Toll-Like receptor 7 (TLR7) agonist with preferential Type-1 interferon (IFN)-stimulating properties. GSK2245035 has pEC 50 s 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 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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 . 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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. IC50& Target:TLR7 IFNα 9.3 (pEC 50 ) CD40 6.5 (pEC 50 ) |
| Canonical SMILES | CCCC(C)OC1=NC(=C2C(=N1)N(C(=O)N2)CCCCCN3CCCCC3)N |
|---|---|
| 分子量 | 390.52 |
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