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- IT3210
- 2025年07月23日
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- 详细信息
- 技术资料
- 保存条件：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
TLR7 agonist 2
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
1642857-69-9
- 规格：
5mg/1mg
| 规格： | 5mg | 产品价格： | ￥4478.0 |
|---|---|---|---|
| 规格： | 1mg | 产品价格： | ￥1490.0 |
| 基本信息 | |
| CAS | No.1642857-69-9 |
| 英文名称 | TLR7 agonist 2 |
| 分子式 | C17H16N6O2 |
| 分子量 | 336.35 |
| 溶解性 | Soluble in DMSO |
| 纯度 | ≥98% |
| 外观(性状) | Solid |
| 储存条件 | Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| SMILES | CC1=CC(=NO1)COC2=NC(=NC3=C2N(C=C3)CC4=CC=CC=N4)N |
| InChIKey | FVKOYFLAKSGBBV-UHFFFAOYSA-N |
| InChI | InChI=1S/C17H16N6O2/c1-11-8-13(22-25-11)10-24-16-15-14(20-17(18)21-16)5-7-23(15)9-12-4-2-3-6-19-12/h2-8H，9-10H2，1H3，(H2，18，20，21) |
| PubChem CID | 86346192 |
| 靶点 | TLR7 |
| 通路 | Immunology & Inflammation |
| 背景说明 | TLR7 agonist 2 是一种有效且有选择性的 Toll 样受体 7 (TLR7) 激动剂。 |
| 生物活性 | TLR7 agonist 2 is a potent and selective Toll-like Receptor 7 (TLR7) agonist with a LEC of 0.4 μM.[1] |
| IC50 | LEC: 0.4 μM (TLR7)[1] |
| In Vitro | TLR7 agonist 2 is a potent and selective Toll-like Receptor 7 (TLR7) agonist with a lowest effective concentration (LEC) of 0.4 μM in HEK293 cell. TLR7 agonist 2 is found to be selective for TLR7 over TLR8 with LEC of >100 μM for human TLR8. TLR7 agonist 2 demonstrates low inhibition across five CYP450 isozymes (IC50 >10 μM) and is also not a time dependent inhibitor of CYP450 3A4. TLR7 agonist 2 has limited inhibition of the hERG potassium ion channel 3H-dofetilide binding in vitro (IC50 >50 μM)[1]. |
| 细胞实验 | TLR7 agonist 2 is found to be rapidly cleared in conjunction with our target profile. Both Cmax and AUC increase less than dose proportionally between 0.3 and 3 mg/kg and more than dose-proportionally between 3 and 10 mg/kg. TLR7 agonist 2 can induce an antiviral interferon stimulated gene (ISG) response without inducing an IFNα response at a low dose. TLR7 agonist 2 also induces a 2.7 log decrease in serum HBV viral load from 0.3 mg/kg， and a maximum 3.1 log decrease is observed for doses between 1 and 5 mg/kg[1]. |
| 细胞实验 | The ability of TLR7 agonist 2 to activate human TLR7 and/or TLR8 is assessed by using HEK293 cells. Briefly， HEK293 cells are grown in culture medium (DMEM supplemented with 10% FCS and 2 mM Glutamine). Transfected cells are then detached with Trypsin-EDTA， washed in PBS and resuspended in medium to a density of 1.67×105 cells/mL. Thirty microliters of cells are then dispensed into each well in 384-well plates， where 10 μL of TLR7-agonist-1 in 4% DMSO is already present. Following 6 hours incubation at 37°C， 5% CO2， the luciferase activity is determined by adding 15 μL of Steady Lite Plus substrate to each well and readout performed on a microplate imager. Lowest effective concentrations (LEC) values are determined for TLR7-agonist-1[1]. |
| 动物实验 | A mouse in vivo model is used to demonstrate the initial proof of concept to induce endogenous IFNα. Single oral administration of 0.3， 1， 3， and 10 mg/kg doses of TLR7 agonist 2 is given to healthy， female， fasted C57Bl/6 mice. Concentrations of TLR7 agonist 2 and mouse-IFN via ELISA are measured from the plasma and compare to vehicle[1]. |
| 数据来源文献 | [1]. McGowan DC， et al. Identification and Optimization of Pyrrolo[3，2-d]pyrimidine Toll-like Receptor 7 (TLR7) Selective Agonists for the Treatment of Hepatitis B. J Med Chem. 2017 Jul 27;60(14):6137-6151. |
| 单位 | 瓶 |
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IT3210 TLR7 agonist 2 免疫学/炎症 索莱宝
￥1490 - 4478
